1000 Sentences With "agonist" | Random Sentence Generator

I thought we were going backwards in treatment from partial agonist to full agonist.

Supporting muscles called "synergists" help the agonist muscles, which are cued by the brain to take on the additional workload if an agonist muscle fails to fire correctly.

Animals that got Gilead's TLR-7 agonist saw no benefit and the virus quickly rebounded.

" As Jacobs put it, "Nobody except WADA seemed to believe Higenamine is a beta2-Agonist.

As a full agonist, methadone doesn't require someone to be in withdrawal to start treatment.

Varenicline (sold under the brand name Chantix), Jani explained, is a nicotinic receptor partial agonist.

However, it does respond to agonist treatment with buprenorphine and methadone, and to injectable naltrexone.

Vancouver PD has also been very forward-thinking when it comes to offering alternative agonist therapies.

Xultophy, approved in Europe since 2014, combines Novo's insulin drug Tresiba with its GLP-1 agonist Victoza.

It could follow up with other NASH drugs — FXR agonist GS-203 and ACC inhibitor GS-0976.

Furthermore, WADA's spokesman reiterated their position that Higenamine is a beta21-agonist, stating "There have been publications describing higenamine as a beta-22-agonist since the late 23s" and that Higenamine has been considered a banned substance since 2004, or as long as WADA has had a banned list.

Activation of the mu opioid receptor by an opioid agonist may cause analgesia, the inability to feel pain.

Fortunately, since a newborn doesn't have the psychological addiction to strong-agonist opioids, buprenorphine has proven a preferable route.

IDegLira combines Novo Nordisk's diabetes drug Tresiba, also known as insulin degludec, with its GLP-1 agonist Victoza, or liraglutide.

The drug combines Novo's drug Tresiba, known also as insulin degludec, with its GLP-1 agonist Victoza, known also as liraglutide.

"We need a model whereby patients can get immediate access to opioid-agonist treatment, a lifesaving intervention, without obstacles," she said.

This is known as injectable opioid agonist treatment, which is different from safe supply programs in that it's more tightly regimented.

They ruled that there are "significant doubts" as to whether Higenamine is a beta23-agonist, a direct contradiction of WADA's position.

He started Agonist with his own money after failing to raise private investment due to scepticism the cafe would be a success.

Kobilka's final conclusion: no proper study has been done on humans which can definitively say that Higenamine acts as a beta2-Agonist.

A couple of months ago, I began taking a new one called a dopamine agonist, which sells under the brand name Neupro.

Buprenorphine is a partial agonist, with a ceiling on its effect that subsequently makes it much harder to misuse or overdose on.

The basic mechanism of opioid drugs, whether it be heroin or fentanyl, is working as an agonist at the mu opioid receptors (MOR).

Buprenorphine is an opioid partial agonist, which means it can produce opioid-like effects, but those effects reach a maximum, and then plateau.

The other main thing we get wrong is the enormous stigma against opioid agonist therapy [such as methadone and buprenorphine] for opioid addiction.

And when patients are using agonist therapies, Teitelbaum—who also was treated for cocaine and marijuana use—said he isn't sure it is.

THC, explains Earleywine, is a partial agonist of the CB1 receptor, which means it binds to that receptor and causes it to fire differently.

Another data point that stands out is the alarming level of exposure to buprenorphine, a "partial-agonist" opioid used to wean addicts off opiates.

Stronger support for syringe access programs and opioid agonist therapy services are a necessary piece of the puzzle to prevent new viral hepatitis infections.

Rather, agonist treatment with buprenorphine or methadone is considered to be first-line, and is often undermined by tactics that highlight detoxification as treatment.

One of the studies concluded Higenamine is primarily a beta228-agonist, which, again is not banned by WADA, and thus directly undermines WADA's own case.

Xultophy, approved in Europe since 2014, combines Novo's drug Tresiba, known also as insulin degludec, with its GLP-1 agonist Victoza, known also as liraglutide.

The authors conclude that, despite the possibly positive effects of marijuana legalization for the general population, patients receiving opioid agonist therapy may be negatively impacted.

China is the world's biggest consumer of pork but strictly enforces a ban on the beta-agonist ractopamine - a feed additive used to plump up pigs.

Simply as a scientific point, the panel couldn't determine whether or not Higenamine is a beta2-Agonist at all—or whether it had performance-enhancing effects.

Many of the studies on Higenamine have been done on rodents, and most determined that Higenamine is a beta1-agonist, which is not banned by WADA.

Duaklir, a combination of the long-acting muscarinic antagonist (LAMA) aclidinium bromide and long-acting beta-agonist (LABA) formoterol fumarate, was approved in Europe in November 2014.

But China has zero tolerance on the use of growth promoter beta-agonist ractopamine, widely used by U.S. pork farmers, and synthetic hormones used in U.S. beef.

But the data at this point is just overwhelming that somebody with severe opioid addiction, if you get them on opioid agonist therapy, their lives are vastly better.

A 2008 study on rodents raised the possibility that Higenamine is also a beta2-agonist, but added the caveat that this effect was "extremely weak," as Morgan put it.

"This is the first orally-available GLP-1 (glucagon-like peptide-1) receptor agonist and that's a pretty big deal," Husain said, noting the fear many patients have for injections.

"The novel triple GLP-1/GIP/Gcg receptor agonist holds clear promise of being developed into a new treatment for chronic neurodegenerative disorders such as Alzheimer's disease," the authors concluded.

The new drug, which is inhaled through a palm-sized device called Ellipta, consists of a corticosteroid to reduce inflammation and a long-acting beta-agonist to open the airways.

But that's in part because they're less risky: Methadone is a full agonist, meaning it fully activates opioid receptors in the brain, which carries a risk of addiction and overdose.

The company's medicine, which is inhaled through a palm-sized device called Ellipta, consists of a corticosteroid to reduce inflammation and a long-acting beta-agonist to open the airways.

For example, exercise induced asthma is a common condition in many athletes, yet WADA bans many of the kinds of beta-2 agonist drugs athletes would take to relieve that condition.

Sublocade is the first once-monthly injectable buprenorphine product — an opioid partial agonist, which produces some opioid-like effects such as euphoria in order to essentially wean someone from true opioids.

International addiction experts consider initial opioid-agonist treatment, or OAT, with no duration restrictions, the evidence-based standard of care for opioid-use disorder, the authors write in Annals of Internal Medicine.

There's evidence to suggest that the hallucinogenic in ayahuasca, DMT, "may function as indirect antioxidants" and can mitigate cellular stress—which is associated with cancerous tumors—as a sigma-1 receptor agonist.

In the notification, UEFA told Sakho that the violation occurred because WADA's prohibited list includes all beta2-agonists, which can be found in asthma inhalers, and that Higenamine is a beta2-agonist.

If those succeed, Novartis would conduct Phase III studies of emricasan and begin development of the drug in combination with its own experimental treatment for chronic liver disease, known as an FXR agonist.

On May 25 the advisory committee will consider a similar drug, Sanofi SA's iGlarLixi, which combines the company's experimental GLP-1 agonist lixisenatide with its insulin treatment Lantus, also known as insulin glargine.

"There's still a tremendous amount of stigma among patients and in communities about taking any opioid agonist in treatment," Chinazo Cunningham, MD, associate chief of general internal medicine at Montefiore Medical Center, told STAT.

He could try Suboxone, a long-acting partial opioid agonist that would not require daily reporting to a clinic, like he had to do for methadone, and he could leave the prison on the medication.

They combined this with Gilead's experimental drug called GS-986, a so-called TLR-7 agonist that kickstarts the innate immune system, a more generalized line of defense that mounts the body's initial response to infection.

"If you offer opioid-agonist treatment from the outset, people live longer, and they incur lower costs on society," said senior author Bohdan Nosyk, a health economist and professor at Simon Fraser University in Vancouver, British Columbia.

An editorial accompanying the study says it adds to decades of data on the efficacy of opioid agonists and should lead policymakers to spend fewer healthcare resources on medically supervised withdrawal and more on opioid-agonist treatment.

They then divided the group into four arms, with one getting the Ad26/MVA vaccine alone, another getting the TLR-7 agonist alone, a third getting the combination of the two, and a fourth getting a placebo.

Prior to her gambling addiction, Sommerville suffered from restless leg syndrome, and studies have shown that the medication prescribed for this, a dopamine agonist, can cause compulsive behavior in up to 20% of people who take them.

Every major public health organization — the Centers for Disease Control and Prevention, the National Institute on Drug Abuse, the American Medical Association, and the World Health Organization — considers opioid agonist treatment a vital approach for combating addiction.

The database included 1,580 reports of impulse control problems resulting from prescribed drugs, split into the following categories: As it turned out, 710 of these reports — about 45 percent — were linked to one of six dopamine agonist drugs.

Maze of Mara Synth-driven metalcore in the vein of Lacuna Coil and The Agonist, Maze of Mara build on an accessible hard rock base to mimic a sound that sees their European counterparts flirt with chart success.

Second, he "questioned the steps that WADA has taken to reach its conclusion" that Higenamine was a beta2-Agonist, alleging that WADA went through none of the four required administrative steps to add a substance to the banned list.

" The FDA considers the drug's impact on children's bones an unanswered question, according to a statement: "The effects of bone density in children whose central precocious puberty is arrested with a GnRH agonist are considered 'unknown' as they have not been studied.

NKTR-214, a CD122 agonist that utilizes the interleukin-2 (IL-2) pathway, is designed to increase the number and activation state of cancer-fighting T cells in the tumor microenvironment, while limiting IL-2 toxicity, with the hope of improving and lengthening patient responses.

"This substance works as an opioid receptor agonist and has been shown to potentially cause several unwanted side effects including hallucinations, depression, chills, and seizures," says Eyvazzadeh, adding that it's difficult to be sure exactly what you're consuming as kratom is an unregulated substance.

One reason for this is that THC acts as a partial agonist, meaning that when it binds to a receptor, it only produces some of the drug's effects, making it less potent than synthetic strains of marijuana like Spice and K2, which are full agonists.

While Orexin-A, an agonist, works by binding to receptors in the brain, Belsomra is an antagonist drug: it blocks molecules from binding at those receptors, and can be used to treat symptoms of insomnia, a sleep disorder that can be called the opposite of narcolepsy.

If the nearly 47,000 Californians who began treatment for opioid-use disorder in 2014 had received immediate access to methadone or another opioid-agonist treatment – instead of first being forced to completely withdraw from opioids – the healthcare and criminal-justice systems would have saved $3.8 billion, researchers estimate.

An irreversible agonist is a type of agonist that binds permanently to a receptor in such a manner that the receptor is permanently activated. It is distinct from a mere (reversible) agonist in that the association of an agonist to a receptor is reversible, whereas the binding of an irreversible agonist to a receptor is, at least in theory, irreversible. Oxymorphazone is an example of an irreversible agonist. In practice, the distinction may be more a matter of degree, in which the binding affinity of an irreversible agonist is some orders of magnitude greater than that of an agonist.

Dose response curves of a full agonist, partial agonist, neutral antagonist, and inverse agonist In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either. Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists. A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand.

Agonists activating hypothetical receptors. An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist.

Cafestol found in coffee is also an agonist. Forskolin is another case example of a PXR agonist.

An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level. The efficacy of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., negative) efficacy.

Agonist vs. antagonist In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, behaves as an antagonist (a substance that binds to a receptor but does not activate and can block the activity of other agonists). Types of mixed agonist/antagonist include receptor ligands that act as agonist for some receptor types and antagonist for others or agonist in some tissues while antagonist in others (also known as selective receptor modulators).

Potency is the amount of agonist needed to elicit a desired response. The potency of an agonist is inversely related to its EC50 value. The EC50 can be measured for a given agonist by determining the concentration of agonist needed to elicit half of the maximum biological response of the agonist. The EC50 value is useful for comparing the potency of drugs with similar efficacies producing physiologically similar effects.

GABOB is a GABA receptor agonist. It has two stereoisomers, and shows stereoselectivity in its actions. Specifically, (R)-(–)-GABOB is a moderate-potency agonist of the GABAB receptor, while (S)-(+)-GABOB is a partial agonist of the GABAB receptor and an agonist of the GABAA receptor. (S)-(+)-GABOB is around twice as potent an anticonvulsant as (R)-(–)-GABOB.

Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also has high affinity for the DOR.

Central dopaminergic agonist properties of semisynthetic ergoline derivatives lergotrile, pergolide, bromocriptine and lisuride have been established. Some studies suggest that ergot alkaloids have the properties of mixed agonist-antagonist with regards to certain presynaptic and postsynaptic receptors. N-n-Propyl groups (chemical formula: –CH2CH2CH3) frequently enhance dopamine agonist effects in the ergoline derivatives.Bromocriptine The (+)-enantiomer displays notably diminished activity whereas the (-)-enantiomer possess potent dopamine agonist properties.

CPA should be given continuously for at least a week prior to GnRH agonist initiation for an optimal preventative effect on the GnRH agonist-induced testosterone flare.

Mixed agonist/antagonist and partial agonist opioids may reduce the analgesic effect of benzhydrocodone/APAP or cause withdrawal symptoms. MAOIs can increase the effects of benzhydrocodone/APAP.

It has been reported that, after prolonged receptor exposure to the agonist, the agonist itself causes an agonist-induced conformational change in the receptor, resulting in receptor desensitisation. Desensitised receptors can revert to a prolonged open state when an agonist is bound in the presence of a positive allosteric modulator, for example PNU-120596. Also, there is evidence that indicates specific chaperone molecules have regulatory effects on these receptors.

2-Aminoethoxydiphenyl borate (2-APB) is a mixed agonist-antagonist of the TRPV3 receptor, acting as an antagonist at low concentrations but showing agonist activity when used in larger amounts. Drofenine also acts as a TRPV3 agonist in addition to its other actions. Conversely, icilin has been shown to act as a TRPV3 antagonist, as well as a TRPM8 agonist. Forsythoside B acts as a TRPV3 inhibitor among other actions.

CP 55,244 is a chemical compound which is a cannabinoid receptor agonist. It has analgesic effects and is used in scientific research. It is an extremely potent CB1 full agonist with a Ki of 0.21 nM, making it more potent than the commonly used full agonist HU-210.

Similarly to related drugs like DOM, DOET likely acts as a 5-HT2A, 5-HT2B, and 5-HT2C receptor partial agonist. It is an agonist of human TAAR1.

Oxymorphone-3-methoxynaltrexonazine (OM-3-MNZ) is a morphinan-based opioid that acts as a selective μ-opioid receptor agonist, unlike the closely related mixed agonist-antagonist Oxymorphonenaltrexonazine.

Saroglitazar is novel first in class drug which acts as a dual PPAR agonist at the subtypes α (alpha) and γ (gamma) of the peroxisome proliferator-activated receptor (PPAR). Agonist action at PPARα lowers high blood triglycerides, and agonist action on PPARγ improves insulin resistance and consequently lowers blood sugar.

The triptan eletriptan is an agonist of the 5-HT1E receptor. BRL-54443 is a selective 5-HT1E and 5-HT1F receptor agonist which is used in scientific research.

The (3R,4R) isomer is the agonist, while (3S,4S) is antagonist.Froimowitz M, Cody V. Absolute configurations and conformations of the opioid agonist and antagonist enantiomers of picenadol. Chirality. 1995;7(7):518-25. This means that the racemic mix of the two enantiomers is a mixed agonist-antagonist, with relatively low abuse potential, and little of the κ-opioid activity that tends to cause problems with other opioid mixed agonist-antagonists such as pentazocine.

L-Glutamic acid (glutamate), the major endogenous agonist of the main site of the NMDAR. Glycine, the major endogenous agonist of the glycine co-agonist site of the NMDAR. Activation of NMDA receptors requires binding of glutamate or aspartate (aspartate does not stimulate the receptors as strongly). In addition, NMDARs also require the binding of the co-agonist glycine for the efficient opening of the ion channel, which is a part of this receptor.

Acetylcholine - the natural agonist of muscarinic and nicotinic receptors. Muscarine - an agonist used to distinguish between these two classes of receptors. Not normally found in the body. Atropine - an antagonist.

CPD-1 (LS-193743) is a drug with a benzofuranyl piperazine structure, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity and full agonist efficacy at the 5-HT2C subtype, and lower affinity and partial agonist action at the 5-HT2A and 5-HT2B subtypes.

General pathways for GPCR homologous desensitization Homologous desensitization occurs when a receptor decreases its response to an agonist at high concentration. It is a process through which, after prolonged agonist exposure, the receptor is uncoupled from its signaling cascade and thus the cellular effect of receptor activation is attenuated. Homologous desensitization is distinguished from heterologous desensitization, a process in which repeated stimulation of a receptor by an agonist results in desensitization of the stimulated receptor as well as other, usually inactive, receptors on the same cell. They are sometimes denoted as agonist-dependent and agonist-independent desensitization respectively.

3-PPP (N-n-propyl-3-(3-hydroxyphenyl)piperidine) is a mixed sigma σ1 and σ2 receptor agonist (with similar affinity for both subtypes, though slightly higher affinity for the latter) and D2 receptor partial agonist which is used in scientific research. It shows stereoselectivity in its pharmacodynamics. (+)-3-PPP is the enantiomer that acts as an agonist of the sigma receptors; it is also an agonist of both D2 presynaptic and postsynaptic receptors. Conversely, (–)-3-PPP, also known as preclamol (), acts as an agonist of presynaptic D2 receptors but as an antagonist of postsynaptic D2 receptors, and has antipsychotic effects.

Examples include denopamine, dobutamine, xamoterol, and epinephrine. Epinephrine is a non- selective beta agonist, this means it also stimulates the beta 2 adrenergic receptor. Therefore, epinephrine is a Beta2-adrenergic agonist.

Bremelanotide is a non-selective agonist of the melanocortin receptors, MC1 through MC5 (with the exception of MC2, the receptor of ), but acting primarily as an MC3 and MC4 receptor agonist.

In pharmacology, an indirect agonist or indirect-acting agonist is a substance that enhances the release or action of an endogenous neurotransmitter but has no specific agonist activity at the neurotransmitter receptor itself. Indirect agonists work through varying mechanisms to achieve their effects, including transporter blockade, induction of transmitter release, and inhibition of transmitter breakdown.

DOB is a 5-HT2A, 5-HT2B, and 5-HT2C receptor agonist or partial agonist. Its psychedelic effects are mediated by its agonistic properties at the 5-HT2A receptor. Due to its selectivity, DOB is often used in scientific research when studying the 5-HT2 receptor subfamily. It is an agonist of human TAAR1.

O-806 is a drug which is a cannabinoid derivative that is used in scientific research. It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co-administered alongside a more potent CB1 agonist, but exhibits weak partial agonist effects when administered by itself.

O-823 is a drug which is a cannabinoid derivative that is used in scientific research. It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co-administered alongside a more potent CB1 agonist, but exhibits weak partial agonist effects when administered by itself.

Guanfacine is a highly selective agonist of the α2A adrenergic receptor, with low affinity for other receptors. However, it may also be a potent 5-HT2B receptor agonist, potentially contributing to valvulopathy.

In pharmacology, an endogenous agonist for a particular receptor is a compound naturally produced by the body which binds to and activates that receptor. For example, the primary endogenous agonist for serotonin receptors is serotonin, and the primary endogenous agonist for dopamine receptors is dopamine.Goodman and Gilman's Manual of Pharmacology and Therapeutics. (11th edition, 2008). p14.

This will often cause the orthosteric site to also change, which can alter the effect of an agonist binding. Allosteric modulators can also stabilize one of the normal configurations of a receptor. In practice, modulation can be complicated. A modulator may function as a partial agonist, meaning it doesn't need the agonist it modulates to yield agonistic effects.

Camicinal is a motilin agonist for the treatment of gastroparesis.

SR3335 has also been discovered as a RORα inverse agonist.

Immethridine is a histamine agonist selective for the H3 subtype.

Isoguvacine is a GABAA receptor agonist used in scientific research.

High concentration of an antagonist can completely inhibit the response. This inhibition can be reversed, however, by an increase of the concentration of the agonist, since the agonist and antagonist compete for binding to the receptor. Competitive antagonists, therefore, can be characterized as shifting the dose–response relationship for the agonist to the right. In the presence of a competitive antagonist, it takes an increased concentration of the agonist to produce the same response observed in the absence of the antagonist.

This model was arguably flawed in that it did not incorporate the equilibrium between the inactivated agonist-bound-receptor and the activated agonist-bound-receptor that is shown in the del Castillo Katz model.

OUP-16 is a histamine agonist selective for the H4 subtype.

The primary endogenous agonist of the human CB1 receptor is anandamide.

4-Methylhistamine is a histamine agonist selective for the H4 subtype.

Potent and selective agonist and antagonists for C5aR have been developed.

Poneratoxin is considered as a slow acting agonist for smooth muscles.

VUF-8430 is a histamine agonist selective for the H4 subtype.

For instance, methamphetamine acts as an agonist of sigma-1 receptor.

5-APB is also an agonist of the 5-HT2C receptor.

Alniditan is a 5-HT1D receptor agonist with migraine-preventive effects.

Whereas nalbuphine must be injected every 4 to 6 hours, a single injection of DNS lasts for up to 7 to 10 days. Nalbuphine, and hence DNS, acts as a mixed agonist/antagonist opioid modulator, or more specifically as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor and as a high-efficacy partial agonist of the κ-opioid receptor.

An opioid modulator (or opioid receptor modulator) is a drug which has mixed agonist and antagonist actions at different opioid receptors and thus cannot clearly be described as either an opioid agonist or antagonist. An example of an opioid modulator is buprenorphine, which is a partial agonist of the μ-opioid receptor and an antagonist of the κ-opioid receptor.

Mitragynine pseudoindoxyl is a μ opioid receptor agonist and δ opioid receptor antagonist and acts as a G protein biased agonist at μ opioid receptors and possesses a favourable side effect profile compared to conventional opioids.

SKF-89,145 is a drug which acts as a dopamine agonist selective for the D1 subtype. The N-desmethyl derivative SKF-89,626 is also a selective D1 agonist with similar potency and selectivity to SKF 89,145.

An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis. In a mouse model of infarction the A3 selective agonist CP-532,903 protected against myocardial ischemia and reperfusion injury.

Modulator may also act as an agonist and yield an agonistic effect (3). Modulated orthosteric agonist affects the receptor (4). Receptor response (F) follows. The site to which endogenous agonists bind to is named the orthosteric site.

Sodelglitazar, formerly known as GW 677954, is a thiazole PPARδ receptor agonist developed by GlaxoSmithKline. While it is primarily active at the PPARδ receptor, it is considered a pan agonist with activity at PPARα and PPARγ receptors.

In rats tolerance is slower to develop to the anticonvulsant effects compared to the benzodiazepine site full agonist diazepam. However, tolerance developed to the anticonvulsant effects of bretazenil partial agonist more quickly than they developed to imidazenil.

Proligestone is a progestogen, or an agonist of the progesterone receptor (PR).

As a glucocorticoid, rimexolone acts as an agonist of the glucocorticoid receptor.

"Halostachine" was thus interpreted as having partial agonist properties at β2 receptors.

When the agonist muscle is inhibited from contracting, the antagonist muscle contracts.

AR-231,453 is an agonist for the suggested novel cannabinoid receptor GPR119.

Prenalterol is a cardiac stimulant which acts as a β1 adrenoreceptor agonist.

Carbuterol (INN; carbuterol hydrochloride USAN) is a short-acting β2 adrenoreceptor agonist.

Thiomuscimol is a GABAA receptor agonist which is structurally related to muscimol.

PWZ-029 is a benzodiazepine derivative drug with nootropic effects developed by WiSys,US Patent application US2006/258643 A1 It acts as a subtype- selective, mixed agonist-inverse agonist at the benzodiazepine binding site on the GABAA receptor, acting as a partial inverse agonist at the α5 subtype and a weak partial agonist at the α3 subtype. This gives it a mixed pharmacological profile, producing at low doses memory-enhancing effects but with no convulsant or anxiogenic effects or muscle weakness, although at higher doses it produces some sedative effects.

Alissa White-Gluz performing with The Agonist in July 2012 In 2004, White-Gluz formed the Agonist (then known as "Tempest") with fellow band members Danny Marino and Chris Kells in Montreal, Quebec, Canada. She released three albums with them as their lead vocalist. White-Gluz left the Agonist in the spring of 2014 after she was offered the role as vocalist for Arch Enemy.

Brimonidine is an α2 adrenergic agonist. α2 agonists, through the activation of a G protein-coupled receptor, inhibit the activity of adenylate cyclase. This reduces cAMP and hence aqueous humour production by the ciliary body. Peripheral α2 agonist activity results in vasoconstriction of blood vessels (as opposed to central α2 agonist activity that decreases sympathetic tone, as can be seen by the medication clonidine).

Competitive antagonists bind to receptors at the same binding site (active site) as the endogenous ligand or agonist, but without activating the receptor. Agonists and antagonists "compete" for the same binding site on the receptor. Once bound, an antagonist will block agonist binding. Sufficient concentrations of an antagonist will displace the agonist from the binding sites, resulting in a lower frequency of receptor activation.

Agonists In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine.

Dimaprit is a histamine analog working as a selective H2 histamine receptor agonist.

2-Pyridylethylamine is a histamine agonist which is selective for the H1 subtype.

Daidzein has been found to act as an agonist of the GPER (GPR30).

TRIMU 5 is a selective agonist of the mu opioid receptor type 2.

It has also been found to be a GABAA receptor agonist in vitro.

Buphenine (or nylidrin) is a β2 adrenoreceptor agonist that acts as a vasodilator.

As such, it is a potent ERβ agonist with high affinity and selectivity.

S-15535 is a phenylpiperazine drug which is a potent and highly selective 5-HT1A receptor ligand that acts as an agonist and antagonist (weak partial agonist) at the presynaptic and postsynaptic 5-HT1A receptors, respectively. It has anxiolytic properties.

A proof of concept study of the farnesoid X receptor agonist obeticholic acid has shown clinical and biochemical benefit. As of March 15, 2016, Novartis Pharmaceuticals is conducting a phase II clinical study involving a farnesoid X receptor agonist named LJN452.

The chemical structure of Mirabegron, a β3-adrenergic receptor agonist. The β3 (beta 3) adrenergic receptor agonist or β3-adrenoceptor agonist, also known as β3-AR agonist, are a class of medicine that bind selectively to β3-adrenergic receptors. β3-AR agonists for the treatment of obesity and type 2 diabetes have been in developmental stages within many large pharmaceutical companies since the early 1990s with without successfully delivering an anti-obesity product to the market. More recently pharmaceutical companies have developed selective β3-AR agonists targeted at urinary inconsistencies and in 2012 Mirabegron (trade name Myrbetriq and Betmiga) was the first β3-AR agonist to be approved in the United States and Europe for the treatment of overactive bladder (OAB) syndrome.

Although estriol is an efficacious agonist of the ERs, it is reported to have mixed agonist–antagonist (partial agonist) activity at the ER; on its own, it is weakly estrogenic, but in the presence estradiol, it is antiestrogenic. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol. It is notable that unlike estriol, estrone can be metabolized into estradiol, and most of its potency in vivo is in fact actually due to conversion into estradiol. In addition to acting as an agonist of the nuclear ERs, estriol at high concentrations (~1,000–10,000 nM) also acts as an antagonist of the GPER, a membrane estrogen receptor where, conversely, estradiol acts as an agonist.

Rose aided in the conception of varenicline for smoking cessation: In the 1990s Rose et al. conducted clinical trials of an agonist-antagonist combination treatment, using nicotine (agonist) and mecamylamine (nicotinic antagonist). The combination proved more efficacious than either agent alone. Pfizer pharmaceuticals cited this work as helping to inspire the development of the partial nicotinic agonist varenicline, which is currently the most effective pharmacologic smoking cessation treatment available.

Antidopaminergic ergolines have found use in antiemetics and in the treatment of schizophrenia. These substances are neuroleptic and are either an antagonist of dopamine at the postsynaptic level at the D2 receptor site or an agonist of dopamine at the presynaptic level at the D1 receptor site. The antagonist or agonist behavior of the ergolines are substrate dependent and mixed agonist/antagonist behaviors of ergoline derivatives have been reported.

Uncompetitive antagonists differ from non-competitive antagonists in that they require receptor activation by an agonist before they can bind to a separate allosteric binding site. This type of antagonism produces a kinetic profile in which "the same amount of antagonist blocks higher concentrations of agonist better than lower concentrations of agonist". Memantine, used in the treatment of Alzheimer's disease, is an uncompetitive antagonist of the NMDA receptor.

An irreversible antagonist binds so strongly to the receptor as to render the receptor unavailable for binding to the agonist. Irreversible antagonists may even form covalent chemical bonds with the receptor. In either case, if the concentration of the irreversible antagonist is high enough, the number of unbound receptors remaining for agonist binding may be so low that even high concentrations of the agonist do not produce the maximum biological response.

Uncompetitive antagonists differ from non-competitive antagonists in that they require receptor activation by an agonist before they can bind to a separate allosteric binding site. This type of antagonism produces a kinetic profile in which "the same amount of antagonist blocks higher concentrations of agonist better than lower concentrations of agonist". Memantine, used in the treatment of Alzheimer's disease, is an uncompetitive antagonist of the NMDA receptor.

This action likely does not contribute to the herb's possible sedative effects, which would be expected from an agonist, rather than an inverse agonist, at this particular binding site. Hydrophilic extractions of the herb commonly sold over the counter, however, probably do not contain significant amounts of isovaltrate. Valerenic acid in valerian stimulates serotonin receptors as a partial agonist, including 5-HT5A which is implicated in the sleep-wake cycle.

It is also found in dandelion coffee. It acts as an adenosine receptor agonist.

It has been found to act as an agonist of adiponectin receptor 1 (AdipoR1).

Pregnenolone 16α-carbonitrile (PCN) is a synthetic, steroidal antiglucocorticoid and pregnane X receptor agonist.

The protein encoded by this gene functions as an agonist and is an angiopoietin.

LPK-26 is a potent and selective κ-opioid agonist, and has analgesic effects.

The full mOR agonist pentapeptide DAMGO is also CNS penetrant upon introduction of glycosylation.

Enilospirone (CERM-3,726) is a selective 5-HT1A receptor agonist of the azapirone class.

Pergolide acts as an agonist of dopamine D2 and D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline. Although pergolide is more potent as an agonist of the D2 receptor, it has high D1 receptor affinity and is one of the most potent D1 receptor agonists of the dopamine receptor agonists that are clinically available. The agonist activity of pergolide at the D1 receptor somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease.

The drug is a 4,5-epoxymorphinan derivative, and is structurally unique relative to other KOR agonists. Nalfurafine may be a biased agonist of the KOR or a KOR subtype-selective agonist. Indeed, it has been found to act as a biased agonist of the KOR, preferring activation of β-arrestin signaling in vitro, but paradoxically, β-arrestin appears to be responsible for KOR agonist-induced aversion, and nalfurafine furthermore shows paradoxical effects in vivo that are not consistent with its in vitro profile. As such, more research is needed to clarify the distinct mechanisms and effects of this drug.

N-Arachidonoyl dopamine (NADA) is an endocannabinoid that acts as an agonist of the CB1 receptor and the transient receptor potential V1 (TRPV1) ion channel. NADA was first described as a putative endocannabinoid (agonist for the CB1 receptor) in 2000 and was subsequently identified as an endovanilloid (agonist for TRPV1) in 2002. NADA is an endogenous arachidonic acid based lipid found in the brain of rats, with especially high concentrations in the hippocampus, cerebellum, and striatum. It activates the TRPV1 channel with an EC50 of approximately of 50nM which makes it the putative endogenous TRPV1 agonist.

Lorcaserin is an appetite suppressant and anti-obesity drug which acts as a selective 5-HT2C receptor agonist. meta- Chlorophenylpiperazine (mCPP) is a 5-HT2C-preferring serotonin receptor agonist that induces anxiety and depression and can cause panic attacks in susceptible individuals.

If efficacy is zero, the substance is considered an antagonist. Orthosteric agonist (A) binds to orthosteric site (B) of a receptor (E). Allosteric modulator (C) binds to allosteric site (D). Modulator increases/lowers the affinity (1) and/or efficacy (2) of an agonist.

CP 47,497 or (C7)-CP 47,497 is a cannabinoid receptor agonist drug, developed by Pfizer in the 1980s. It has analgesic effects and is used in scientific research. It is a potent CB1 agonist with a Kd of 2.1 nM.Roger Pertwee. Cannabinoids.

Raloxifene acts as a partial agonist of the ERα and as a pure antagonist of the ERβ. In contrast to the classical ERs, raloxifene is an agonist of the G protein- coupled estrogen receptor (GPER) ( = 10–100 nM), a membrane estrogen receptor.

Telmisartan activates PPAR-δ receptors in several tissues. Also, Telmisartan has a PPARγ agonist activity.

AS-19 is a 5-HT7 receptor agonist that has been used in scientific research.

Zinterol is a beta-adrenergic agonist. Its structure is based on soterenol (antiarrhythmic) and phentermine.

S-14,506 is a phenylpiperazine, a 5-HT1A receptor agonist, and a dopamine receptor antagonist.

The mechanism for this is complex and may be separate from its delta agonist effects.

PB-28 is an agonist of the sigma-2 receptor. It is derived from cyclohexylpiperazine.

Amanita muscaria, which contains ibotenic acid Ibotenic acid acts as a potent agonist of the NMDA and group I (mGluR1 and mGluR5) and II (mGluR2 and mGluR3) metabotropic glutamate receptors. It is inactive at group III mGluRs. Ibotenic acid also acts as a weak agonist of the AMPA and kainate receptors. In addition, due to in vivo decarboxylation into muscimol, it acts indirectly as a potent GABAA and GABAA-ρ receptor agonist.

PNU-22394 is a drug which acts as an agonist at serotonin 5-HT2 receptors, with strongest binding affinity for 5-HT2A and 5-HT2C and slightly weaker at 5-HT2B, although it is only a full agonist at 5-HT2C, but partial agonist at 5-HT2A and 5-HT2B. It has anorectic effects in both animal studies and human trials, along with "Pro-Cognitive Properties", although it has never been developed for medical use.

While competitive antagonists bind to the agonist or ligand binding site of the receptor reversibly, non-competitive antagonists can either bind to the ligand site or other site called the allosteric site. A receptor's agonist does not bind to its allosteric binding site. The binding of a non-competitive antagonist is irreversible. If the non- competitive antagonist binds to the allosteric site and an agonist binds to the ligand site, the receptor will remain unactivated.

An agonist is a chemical capable of binding to a receptor, such as a neurotransmitter receptor, and initiating the same reaction typically produced by the binding of the endogenous substance. An agonist of a neurotransmitter will thus initiate the same receptor response as the transmitter. In neurons, an agonist drug may activate neurotransmitter receptors either directly or indirectly. Direct-binding agonists can be further characterized as full agonists, partial agonists, inverse agonists.

Tetrahydrocannabinol-C4 (Δ9-THCB, (C4)-Δ9-THC, butyl-THC), is a homologue of tetrahydrocannabinol (THC), the active component of cannabis. They are only different by the pentyl side chain being replaced by a butyl side chain. It is unknown whether THCB is an agonist, partial agonist, or antagonist at the cannabinoid receptors. The propyl analog, THCV, is a cannabinoid receptor type 1 and cannabinoid receptor type 2 antagonist, while THC is a CB1 agonist.

This anti- inflammatory action is induced through agonist action at cannabinoid receptors, which prevents microglial activation that elicits the inflammation. Additionally, cannabinoids completely abolish neurotoxicity related to microglial activation in rat models. WIN 55,212-2 is a full agonist at the CB1 cannabinoid receptor (Ki = 1.9 nM) and has much higher affinity than THC (Ki = 41 nM) for this receptor. WIN 55,212-2 is also an agonist of the PPARα and PPARγ nuclear receptors.

In addition to any issues of treatment compliance, and maximised corticosteroids (inhaled or oral) and beta agonist, brittle asthma treatment also involves for type 1 additional subcutaneous injections of beta2 agonist and inhalation of long acting beta-adrenoceptor agonist, whilst type 2 needs allergen avoidance and self-management approaches. Since catastrophic attacks are unpredictable in type 2, patients may display identification of the issue, such as a MedicAlert bracelet, and carry an epinephrine autoinjector.

RDS-127 is a drug which is used in scientific research. It acts as a D2-like receptor agonist and also has some serotonin and adrenergic agonist effects, as well as some anticholinergic action, and produces both anorectic and pro- sexual effects in animal studies.

Sumanirole (PNU-95,666) is a highly selective D2 receptor full agonist, the first of its kind to be discovered.Romero AG, et al. Synthesis of the selective D2 receptor agonist PNU-95666E from D-phenylalanine using a sequential oxidative cyclization strategy. Journal of Organic Chemistry.

Overall signal can be increased by preventing the desensitization of a receptor. Desensitization prevents a receptor from activating, despite the presence of agonist. This is often caused by repeated or intense exposures to agonist. Eliminating or reducing this phenomenon increasing the receptor's overall activation.

Neuromedin U is an agonist at both the NMU1 and NMU2 subtypes, while neuromedin S is selective for NMU2, and is a more potent agonist at this subtype than neuromedin U. Several other peptide and non-peptide ligands are also available for the NMU receptors.

A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its affinity for nicotine. Examples include nicotine (by definition), acetylcholine (the endogenous agonist of nAChRs), choline, epibatidine, lobeline, varenicline and cytisine.

BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist.

Pindolol has modest beta-adrenergic agonist activity and is therefore used with caution in angina pectoris.

Quinelorane is a drug which acts as a dopamine agonist for the D2 and D3 receptor.

Final maturation induction using GnRH agonist results in a substantial decrease in the risk of ovarian hyperstimulation syndrome (OHSS). A Cochrane review estimated that using GnRH agonist instead of hCG in IVF decreases the risk of mild, moderate or severe OHSS with an odds ratio of approximately 0.15. The review estimated that, for a woman with a 5% risk of mild, moderate or severe OHSS with the use of HCG, the risk of OHSS with the use of a GnRH agonist would be between 0 and 2%. However, using GnRH agonist has a lower live birth rate than when using hCG in autologous oocyte transfers (rather than ones using oocyte donation).

Aripiprazole's mode of action differs from other atypical antipsychotics in its selectivity with dopamine receptors (partial agonist activity on postsynaptic D2 receptor and partial agonist activity on presynaptic D2, D3 and partially D4) and serotonin receptors (partial agonist of 5-HT1A and antagonist of 5-HT2A. Aripiprazole's main antagonist action on the dopamine D2 postsynaptic receptor is believed to decrease excessive dopaminergic activity and may also decrease the synthesis and release of dopamine through its presynaptic D2 antagonist action. Furthermore, the drug's agonist activity on seretonin receptor 5-HT1A is believed to possess an anxiolytic effect, providing an possible explanation for the decreased social anxiety patients noticed.

Arachidonyl-2'-chloroethylamide (ACEA) is a synthetic agonist of the CB1 (CB1R). ACEA is considered to be a selective cannabinoid agonist as it binds primarily to the CB1R and has low affinity to the CB2 (CB2R) (Ki = 1.4 nM for CB1R; Ki = 3100 nM for CB2R).

ICI-199,441 is a drug which acts as a potent and selective κ-opioid agonist, and has analgesic effects. It is a biased agonist of the KOR, and is one of a relatively few KOR ligands that is G protein-biased rather than β-arrestin- biased.

Synephrine behaved as a partial agonist at α1A receptors, but as an antagonist at α2A and α2C sub-types. Racemic synephrine has been shown to be an agonist of the TAAR1, although its potency at the human TAAR1 is relatively low (EC50 = 23700 nM; Emax = 81.2%).

AMN082 (N,N'-dibenzhydrylethane-1,2-diamine dihydrochloride) is a selective metabotropic glutamate receptor 7 (mGluR7) allosteric agonist. It mimics the effect of glutamate. AMN082 is the first selective mGluR7 agonist and has expanded the potential array of research opportunities on the effects of mGluR7 in the CNS.

SKF-83,959 is a synthetic benzazepine derivative used in scientific research which acts as an agonist at the D1-D2 dopamine receptor. It behaves as a full agonist at the D1 protomer and a high-affinity partial agonist at the D2 protomer. It was further shown to act as an allosteric modulator of the sigma-1 receptor. SKF-83,959 is a racemate that consists of the R-(+)- and S-(−)-enantiomers MCL 202 and MCL 201, respectively.

The first is an agonist conformation which favors the binding of coactivator proteins which in turn favors upregulation of gene transcription. The second is an antagonistic conformation which in contrast favors the binding of corepressors and as a consequence down regulation of gene expression. Full agonists such as progesterone, which display agonist properties in all tissues, strongly shift the conformational equilibrium in the agonist direction. Conversely full antagonists such as aglepristone strongly shift the equilibrium in the antagonist direction.

6-Br-APB is a synthetic compound that acts as a selective D1 agonist, with the (R)-enantiomer being a potent full agonist, while the (S) enantiomer retains its D1 selectivity but is a weak partial agonist. (R)-6-Br-APB and similar D1-selective full agonists like SKF-81,297 and SKF-82,958 produce characteristic anorectic effects, stereotyped behaviour and self- administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine.

The muscle contraction of a ballistic muscle movement can exhibit a muscle coactivation of concurrent agonist Lee, J.B., Matsumoto, T., Othman, T., Yamauchi, M., Taimura, A., Kaneda, E., Ohwatari, N. and Kosaka, M. (1999) Coactivation of the flexor muscles as a synergist with the extensors during ballistic finger exetension movement in trained kendo and karate athletes. International Journal of Sports Medecine. 20(1): 7-11. and antagonist muscles or the characteristic triphasic agonist/antagonist/agonist muscle activation.

LGD-3303 is a drug which acts as a selective androgen receptor modulator (SARM), with good oral bioavailability. It is a selective agonist for the androgen receptor, producing functional selectivity with effective dissociation of anabolic and androgenic effects, acting as a partial agonist for androgenic effects, but a full agonist for anabolic effects. It has been investigated as a possible treatment for osteoporosis, and was shown in animal studies to enhance the effectiveness of a bisphosphonate drug.

Partial agonists are defined as drugs that, at a given receptor, might differ in the amplitude of the functional response that they elicit after maximal receptor occupancy. Although they are agonists, partial agonists can act as a competitive antagonist in the presence of a full agonist, as it competes with the full agonist for receptor occupancy, thereby producing a net decrease in the receptor activation as compared to that observed with the full agonist alone.Principles and Practice of Pharmacology for Anaesthetists By Norton Elwy Williams, Thomas Norman Calvey Published 2001 Blackwell Publishing Clinically, their usefulness is derived from their ability to enhance deficient systems while simultaneously blocking excessive activity. Exposing a receptor to a high level of a partial agonist will ensure that it has a constant, weak level of activity, whether its normal agonist is present at high or low levels.

On the other hand, Naloxone has no partial agonist effects, and is in fact a partial inverse agonist at μ-opioid receptors, and so is the preferred antidote drug for treating opioid overdose. Naltrexone is also a partial inverse agonist, and this property is exploited in treatment of opioid addiction, as a sustained course of low-dose naltrexone can reverse the altered homeostasis which results from long-term abuse of opioid agonist drugs. This is the only treatment available which can reverse the long-term after effects of opioid addiction known as post acute withdrawal syndrome, which otherwise tends to produce symptoms such as depression and anxiety that may lead to eventual relapse. A course of low-dose naltrexone is thus often used as the final step in the treatment of opioid addiction after the patient has been weaned off the substitute agonist such as methadone or buprenorphine, in order to restore homeostasis and minimize the risk of post acute withdrawal syndrome once the maintenance agonist has been withdrawn.

The key compound in Salvia divinorum, salvinorin A, is known as a powerful, short-acting KOR agonist.

An alternative term is serotonin partial agonist/reuptake inhibitor (SPARI), which can be applied only to vilazodone.

As a glucocorticoid, dexamethasone is an agonist of the glucocorticoid receptor (GR). It has minimal mineralocorticoid activity.

Dimethylglycine has been found to act as an agonist of the glycine site of the NMDA receptor.

SL-75102, or progabide acid, is an active metabolite of progabide and an anticonvulsant GABA receptor agonist.

Another stroke medication trialed at the same time, picozotan, is similar to repinotan in that it is also a serotonin agonist. Other drugs included zonampanel, which acts as an AMPA receptor antagonist instead of a 5-HT1A receptor agonist and DP-b99. DP-b99 is a metal iron chelator.

The neurotransmitter serotonin (illustration) has various receptors. A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors.

Arachidonylcyclopropylamide (ACPA) is a synthetic agonist of the cannabinoid receptor 1 (CB1R). ACPA is considered to be a selective cannabinoid agonist as it binds primarily to the CB1R and has low affinity to the cannabinoid receptor 2 (CB2R) (Ki = 2.2 nM for CB1R; Ki = 700 nM for CB2R).

RCS-4 is a potent cannabinoid receptor agonist, with EC50 values of 146 nM for human CB1 receptors, and 46 nM for human CB2 receptors. All methoxyphenyl regioisomers, and N-butyl homologues of RCS-4 and its regioisomers also display potent agonist activities at CB1 and CB2 receptors.

Dihydromorphine acts as an agonist at the μ-opioid (mu), δ-opioid (delta) and κ-opioid (kappa) receptors. Agonist of the μ-opioid and δ-opioid receptors is largely responsible for the clinical effects of opioids like dihydromorphine with the μ agonism providing more analgesia than the δ.

N-Acetylserotonin (NAS), also known as normelatonin, is a naturally occurring chemical precursor and intermediate in the endogenous production of melatonin from serotonin. It also has biological activity in its own right, including acting as a melatonin receptor agonist, an agonist of the TrkB, and having antioxidant effects.

3-Bromocytisine is a derivative of the toxic alkaloid cytisine that acts as a highly potent agonist at neural nicotinic acetylcholine receptors, binding primarily to the α4β2 and α7 subtypes. 3-Bromocytisine is a full agonist at the α7 subtype while it is only a partial agonist at α4β2, but has an extremely strong binding affinity at α4β2 with 200-fold selectivity for α4β2 over α7. In animal studies 3-bromocytisine stimulates the release of dopamine and noradrenaline and increases locomotor activity.

JWH-051 is an analgesic drug which is a cannabinoid agonist. Its chemical structure is closely related to that of the potent cannabinoid agonist HU-210, with the only difference being the removal of the hydroxyl group at position 1 of the aromatic ring. It was discovered and named after John W. Huffman. JWH-051 retains high affinity for the CB1 receptor, but is a much stronger agonist for CB2, with a Ki value of 14nM at CB2 vs 19nM at CB1.

Cyclorphan is an opioid analgesic of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) weak partial agonist or antagonist, κ-opioid receptor (KOR) full agonist, and, to a much lesser extent, δ-opioid receptor (DOR) agonist (75-fold lower affinity relative to the KOR). The drug was first synthesized in 1964 by scientists at Research Corporation.US Patent 3,285,922Varghese V & Hudlicky T. A Short History of the Discovery and Development of Naltrexone and Other Morphine Derivatives.

5-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with selectivity for the D2 receptor and D3 receptor subtypes. Only the (S)-enantiomer is active as an agonist, with the (R)-enantiomer being a weak antagonist at D2 receptors. Radiolabelled 11C-5-OH-DPAT is used as an agonist radioligand for mapping the distribution and function of D2 and D3 receptors in the brain, and the drug is also being studied in the treatment of Parkinson's disease.

Nalfurafine is an orally active, centrally acting, highly potent, selective full agonist of the κ-opioid receptor (KOR) (Ki = 75 pM; EC50 = 25 pM). As touched on above, nalfurafine shows atypical properties as a KOR agonist relative to other drugs. Notably, it does not completely substitute for the prototypical KOR agonist U-50488 in rodents, indicating qualitative differences in the discriminative effects of the two compounds. Moreover, unlike U-50488, it produces neither conditioned place aversion or preference in rodents.

Nalmefene is a partial agonist of the κ-opioid receptor and may be useful to treat cocaine addiction.

18-Deoxyaldosterone is a steroidal antimineralocorticoid with mixed agonist–antagonist but predominantly antagonistic activity at the mineralocorticoid receptor.

Bamaluzole is a GABA receptor agonist. It was patented as an anticonvulsant by Merck but was never marketed.

Guanfacine may be a 5-HT2B agonist, based on the results of theoretical modeling and high- throughput screening.

L-687,384 is a sigma receptor agonist, selective for the σ1 subtype, as well as an NMDA antagonist.

L-165041 is a phenyloxyacetate PPARδ receptor agonist. It is less potent and PPARδ selective than GW 501516.

GW0742 (also known as GW610742) is a PPARδ/β agonist that is investigated for drug use by GlaxoSmithKline.

Fourphit (4-isothiocyanato-1-[1-phenylcyclohexyl]piperidine) is a covalent binding NMDA antagonist, dopaminergic and sigma receptor agonist.

Nalfurafine, an orally-administered, centrally-acting κ-opioid receptor agonist, is approved to treat the condition in Japan.

Kimball and Murlin coined the term glucagon in 1923 when they initially named the substance the glucose agonist.

Dobutamine is a direct-acting agent whose primary activity results from stimulation of the β1-adrenoceptors of the heart, increasing contractility and cardiac output. Since it does not act on dopamine receptors to inhibit the release of norepinephrine (another α1 agonist), dobutamine is less prone to induce hypertension than is dopamine. Dobutamine is predominantly a β1-adrenergic agonist, with weak β2 activity, and α1 selective activity, although it is used clinically in cases of cardiogenic shock for its β1 inotropic effect in increasing heart contractility and cardiac output. Dobutamine is administered as a racemic mixture consisting of both (+) and (−) isomers; the (+) isomer is a potent β1 agonist and α1 antagonist, while the (−) isomer is an α1 agonist.

Xorphanol (INN) (developmental code name TR-5379 or TR-5379M), also known as xorphanol mesylate (USAN), is an opioid analgesic of the morphinan family that was never marketed. Xorphanol is a mixed agonist–antagonist of opioid receptors, acting preferentially as a high-efficacy partial agonist/near-full agonist of the κ-opioid receptor (Ki = 0.4 nM; EC50 = 3.3 nM; = 49%; = 0.84) and to a lesser extent as a partial agonist of the μ-opioid receptor (Ki = 0.25 nM; IC50 = 3.4 nM; = 29%) with lower relative intrinsic activity and marked antagonistic potential (including the ability to antagonize morphine- induced effects and induce opioid withdrawal in opioid-dependent individuals). The drug has also been found to act as an agonist of the δ-opioid receptor (Ki = 1.0 nM; IC50 = 8 nM; = 76%). Xorphanol produces potent analgesia, and was originally claimed to possess a minimal potential for dependence or abuse.

Therefore, even selective mu agonists can cause analgesia under the right conditions, whereas under others can cause none whatsoever.Alvimopan It is also suggested however that the pain modulated by the μ-opioid receptor and that modulated by the δ-opioid receptor are distinct types, with the assertion that DOR modulates the nociception of chronic pain, while MOR modulates acute pain. Evidence for whether delta agonists produce respiratory depression is mixed; high doses of the delta agonist peptide DPDPE produced respiratory depression in sheep, but in tests on mice the non-peptide delta agonist SNC-80 produced respiratory depression only at the very high dose of 40 mg/kg. In contrast both the peptide delta agonist Deltorphin II and the non-peptide delta agonist (+)-BW373U86 actually stimulated respiratory function and blocked the respiratory depressant effect of the potent μ-opioid agonist alfentanil, without affecting pain relief.

Proxorphan (INN), also known as proxorphan tartate (USAN) (developmental code name BL-5572M), is an opioid analgesic and antitussive drug of the morphinan family that was never marketed. It acts preferentially as a κ-opioid receptor partial agonist and to a lesser extent as a μ-opioid receptor partial agonist.

Oxymetazoline is a selective α1 adrenergic receptor agonist and α2 adrenergic receptor partial agonist. It is a topical decongestant, used in the form of oxymetazoline hydrochloride. It was developed from xylometazoline at E. Merck Darmstadt by Fruhstorfer in 1961.German Patent 1,117,588 Oxymetazoline is generally available as a nasal spray.

A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes. H2 : Betazole and Impromidine are examples of agonists used in diagnostics to increase histamine. H3 : Betahistine is a weak Histamine1 agonist and a very strong Histamine3 antagonist (paradoxically histamine increasing).

AB-PICA is a potent agonist for the CB1 receptor (EC50 = 12 nM) and CB2 receptor (EC50 = 12 nM).

Nelivaptan (SSR149415) and D-[Leu4-Lys8]-vasopressin are a specific antagonist and agonist for the vasopressin 1b receptor, respectively.

MK-9470 is a synthetic compound, which binds to the CB1 cannabinoid receptor and functions as an inverse agonist.

Low- affinity binding (high Ki level) implies that a relatively high concentration of a ligand is required before the binding site is maximally occupied and the maximum physiological response to the ligand is achieved. In the example shown to the right, two different ligands bind to the same receptor binding site. Only one of the agonists shown can maximally stimulate the receptor and, thus, can be defined as a full agonist. An agonist that can only partially activate the physiological response is called a partial agonist.

DREADD agonist 21 (AKA Compound 21) represents an alternative agonist for muscarinic-based DREADDs and an alternative to CNO. It has been reported that DREADD agonist 21 (Compound 21) has excellent bioavailability, pharmacokinetic properties and brain penetrability and does not undergo back metabolism to clozapine. Perlapine, a drug already approved for treating insomnia in Japan is an activator of Gq-, Gi-, and Gs DREADDs that has structural similarity to CNO. Salvinorin B is a brain penetrant, potent and selective activator of κ-opioid DREADD (KORD).

A muscle imbalance between an agonist and antagonist muscle can occur due to a neurological disorder, spinal cord injury, and our lifestyle/postural habits. A decrease in muscle tone leads to continuous disuse and eventually muscular atrophy. The constant contraction of the agonist muscle with minimal resistance can result in a contracture.

Chemical antagonists impede the normal function of a system. They function to invert the effects of other molecules. The effects of antagonists can be seen after they have encountered an agonist, and as a result, the effects of the agonist is neutralized. Antagonists such as dopamine antagonist slow down movement in lab rats.

JWH-030 is a research chemical which is a cannabinoid receptor agonist. It has analgesic effects and is used in scientific research. It is a partial agonist at CB1 receptors, with a Ki of 87 nM, making it roughly half the potency of THC. It was discovered and named after John W. Huffman.

As of 2017, CBC is under laboratory research to identify its possible pharmacological properties. No in vivo human studies exist as of 2019. In vitro, CBC is not active at CB1 or CB2 receptors, but is an agonist of TRPA1 and less potently, an agonist of TRPV3 and TRPV4. CBC has two stereoisomers.

Propylpyrazoletriol (PPT) is a synthetic, nonsteroidal agonist of ERα with 400-fold selectivity over ERβ that is used widely in scientific research to study the function of ERα. Though originally thought to be highly selective for ERα, PPT has subsequently been found to also act as an agonist of the GPER (GPR30).

Adinazolam binds to peripheral-type benzodiazepine receptors that interact allosterically with GABA receptors as an agonist to produce inhibitory effects.

TB-21007 is a nootropic drug which acts as a subtype-selective inverse agonist at the α5 containing GABAA receptors.

Some research suggests dopamine receptor agonist may be effective in treating depression, however studies are few and results are preliminary.

1-PP possesses 5-HT1A partial agonist and α2-adrenergic antagonist actions and likely contributes overall mostly to side effects.

Without these signals, the body overheats. Likewise, this explains the propensity of capsaicin (a TRPV1 agonist) to cause sweating (i.e.

Chloroxymorphamine is an opioid and a derivative of oxymorphone which binds irreversibly as an agonist to the μ-opioid receptor.

Toremifene and fulvestrant are SERMs with little or no agonist activity, and are used for treatment of metastatic breast cancer.

Estropipate is a prodrug of estrone and estradiol. Hence, it is an estrogen, or an agonist of the estrogen receptors.

A study by Fung and colleagues (2017) found no difference in suppression of circulating testosterone levels (~95% suppression) in transgender women by the combination of either 25 mg/day oral CPA or 50 mg/day oral CPA with a moderate dosage of oral or transdermal estradiol (mean 3.3 mg/day oral, 3.4 g/day gel, or 95.6 μg/day patches). A high dosage of CPA given starting 7 days prior to initiation of GnRH agonist therapy was found to prevent the GnRH agonist-induced flare in testosterone levels. The combination of 100 mg/day CPA and 0.1 mg/day diethylstilbestrol given starting 4 weeks before GnRH-agonist introduction has also been found to prevent the GnRH agonist-induced testosterone flare.

The effect of RWJ-394674 when administered in vivo thus produces potent agonist effects at both μ and δ receptors through the combined actions of the parent drug and its active metabolite, with the δ-agonist effects counteracting the respiratory depression from the μ-opioid effects, and the only prominent side-effect being sedation.

Efficacy spectrum of receptor ligands. In the field of pharmacology, a superagonist is a type of agonist that is capable of producing a maximal response greater than the endogenous agonist for the target receptor, and thus has an efficacy of more than 100%. For example, goserelin is a superagonist of the gonadotropin-releasing hormone receptor.

Membranous glomerulonephritis is a serious human disease that can be treated with ACTH, which is a known agonist of MC1R. In a rat model of nephritis it was found that treatment with a different agonist of MC1R improved aspects of kidney morphology and reduced proteinuria, which may help explain the benefit of ACTH in humans.

Psilocin acts as a 5-HT2A, 5-HT2C and 5-HT1A agonist or partial agonist. Receptors are claimed to significantly regulate visuals, decision making, mood, decreased blood pressure and heart rate. There is virtually no direct lethality associated with psilocin. There is virtually no withdrawal syndrome when chronic use of this drug is ceased.

For example, morphine is an agonist of the opioid receptor family. Conversely, antagonists bind to a receptor and elicit no cellular change. Naloxone, an antagonist of the opioid receptors, exerts a biological effect only be interfering with endogenous neurotransmitter (morphine) binding. Inverse agonists bind to receptors and elicit the opposite effect that an agonist would.

DPDPE ([-2,-5]enkephalin) is a synthetic opioid peptide and a selective agonist of the δ-opioid receptor (DOR) which is used in scientific research. It was developed in the early 1980s and was the first highly selective agonist of the DOR to be developed. It was derived from structural modification of met-enkephalin.

These mutants reflect the importance of ABA in seed germination and early embryo development. Pyrabactin (a pyridyl containing ABA activator) is a naphthalene sulfonamide hypocotyl cell expansion inhibitor, which is an agonist of the seed ABA signaling pathway. It is the first agonist of the ABA pathway that is not structurally related to ABA.

NADA also promotes the inflammatory resolution of human endothelial cells activated by both endogenous (i.e. TNF) and exogenous (i.e. bacterial derived LPS (TLR4 agonist) and FSL-1 (TLR2/6 agonist)) inflammatory mediators. It can increase the TRPV1-mediated release of substance P and calcitonin gene-related peptide (CGRP) in rat dorsal spinal cord slices.

Urapidil is a sympatholytic antihypertensive drug. It acts as an α1-adrenoceptor antagonist and as an 5-HT1A receptor agonist. Although an initial report suggested that urapidil was also an α2-adrenoceptor agonist, this was not substantiated in later studies that demonstrated it was devoid of agonist actions in the dog saphenous vein and the guinea-pig ileum. Unlike some other α1-adrenoceptor antagonists, urapidil does not elicit reflex tachycardia, and this may be related to its weak β1-adrenoceptor antagonist activity, as well as its effect on cardiac vagal drive.

AM-411 (part of the AM cannabinoid series) is an analgesic drug that is a cannabinoid agonist. It is a derivative of Δ8-THC substituted with an adamantyl group at the 3-position, demonstrating that the binding pocket for the alkyl chain at this position can accommodate significant bulk. AM-411 is a potent and fairly selective CB1 full agonist with a Ki of 6.80 nM, but is still also a moderately potent CB2 agonist with a Ki of 52.0 nM. It produces similar effects to other cannabinoid agonists such as analgesia, sedation, and anxiolysis.

The condition gradually improves over a period of time which can range from six months to several years in more severe cases. Longer term and heavier use substance abusers have caused damage to the nervous system, where, after cessation of the primary substance of abuse, the opioid receptors may become favorable to any potential agonist. This places longer term and heavier use substance abusers at risk to become addicted to any other agonist with very little use of the secondary agonist. Abstinence from all agonists, sometimes taking multiple years, is required for full recovery.

UH-232 ((+)-UH232) is a drug which acts as a subtype selective mixed agonist- antagonist for dopamine receptors, acting as a weak partial agonist at the D3 subtype, and an antagonist at D2Sh autoreceptors on dopaminergic nerve terminals. This causes dopamine release in the brain and has a stimulant effect, as well as blocking the behavioural effects of cocaine. It may also serve as a 5-HT2A receptor agonist, based on animal studies. It was investigated in clinical trials for the treatment of schizophrenia, but unexpectedly caused symptoms to become worse.

Proxyfan is a histamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from full agonist, to antagonist, to inverse agonist in different tissues, depending on the level of constitutive activity of the histamine H3 receptor. This gives it a complex activity profile in vivo which has proven useful for scientific research.Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM. High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature. 2000 Dec 14;408(6814):860-4.

Structural basis for the mechanism of nuclear receptor agonist and antagonist action. The structures shown here are of the ligand binding domain (LBD) of the estrogen receptor (green cartoon diagram) complexed with either the agonist diethylstilbestrol (top, ) or antagonist 4-hydroxytamoxifen (bottom, ). The ligands are depicted as space filling spheres (white = carbon, red = oxygen). When an agonist is bound to a nuclear receptor, the C-terminal alpha helix of the LDB (H12; light blue) is positioned such that a coactivator protein (red) can bind to the surface of the LBD.

It also has little to no incidence of dysphoria, dissociation, hallucinations, and related side effects at typical therapeutic doses. Nalbuphine is a mixed agonist/antagonist opioid modulator. Specifically, it acts as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor (MOR) and as a high-efficacy partial agonist of the κ-opioid receptor (KOR), whereas it has relatively low affinity for the δ-opioid receptor (DOR) and sigma receptors. Nalbuphine was patented in 1963 and was introduced for medical use in the United States in 1979.

Butorphanol exhibits partial agonist and antagonist activity at the μ-opioid receptor, as well as partial agonist activity at the κ-opioid receptor (Ki = 2.5 nM; EC50 = 57 nM; Emax = 57%). Stimulation of these receptors on central nervous system neurons causes an intracellular inhibition of adenylate cyclase, closing of influx membrane calcium channels, and opening of membrane potassium channels. This leads to hyperpolarization of the cell membrane potential and suppression of action potential transmission of ascending pain pathways. Because of its κ-agonist activity, at analgesic doses butorphanol increases pulmonary arterial pressure and cardiac work.

4-Fluoro-5-Methoxy-N,N-dimethyltryptamine (4-F-5-MeO-DMT) was first described by David E. Nichols team in 2000. It is a potent 5-HT1A agonist. Substitution with the 4-fluorine markedly increased 5-HT1A selectivity over 5-HT2A/2C receptors with potency greater than that of the 5-HT1A agonist 8-OH-DPAT. The analog compound with the N,N-dialkyl substituents constrained into a pyrrolidine ring, is a slightly stronger agonist for the 5-HT1A receptor and retains the selectivity over the 5-HT2A/2C receptors.

LAAM acts as a μ-opioid receptor agonist. It also acts as a potent, noncompetitive α3β4 neuronal nicotinic acetylcholine receptor antagonist.

Memantine acts as an agonist at the dopamine D2 receptor with equal or slightly higher affinity than to the NMDA receptors.

Synergistic muscles aid the agonist muscles in motor control tasks, but they act against excess motion that the agonists may create.

Carazolol is a high affinity antagonist/partial inverse agonist (also referred to as a beta blocker) of the β-adrenergic receptor.

THJ-2201 acts as a full agonist with a binding affinity of 1.34nM at CB1 and 1.32nM at CB2 cannabinoid receptors.

Some unnatural synthetic analogs were also prepared. For example, 1,1-bis(3'-indolyl)-1-(p-methoxyphenyl)methane is a Nur77 agonist.

BB-22 acts as a full agonist with a binding affinity of 0.217nM at CB1 and 0.338nM at CB2 cannabinoid receptors.

Methoxamine is an α1-adrenergic receptor agonist, somewhat similar in structure to butaxamine and 2,5-DMA. It is no longer marketed..

BRL-54443 is a drug which acts as a selective agonist for the 5-HT1E and 5-HT1F serotonin receptor subtypes.

Nabazenil (SP-175) is a synthetic cannabinoid receptor agonist, which has anticonvulsant properties.Concise dictionary of pharmacological agents: properties and synonyms. p188.

The TRPV1 agonist capsaicin, found in chili peppers, has been indicated to relieve neuropathic pain. TRPV1 antagonists inhibit nociception at TRPV1.

WIN 54,461 (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2.

Classical agonist of this receptor includes bradykinin1-8 (bradykinin with the first 8 amino acid) and antagonist includes [Leu8]-bradykinin1-8.

Ketoconazole has been used to prevent the testosterone flare at the initiation of GnRH agonist therapy in men with prostate cancer.

2-Chloro-N6-cyclopentyladenosine (CCPA) is a specific receptor agonist for the Adenosine A1 receptor. It is similar to N6-cyclopentyladenosine.

Methimepip is a histamine agonist which is highly selective for the H3 subtype. It is the N-methyl derivative of immepip.

Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities.

Vicky Psarakis (born June 22, 1988) is a Greek American vocalist, best known as the vocalist of Canadian metal band, the Agonist. She joined in 2014 replacing original vocalist and co-founder Alissa White-Gluz. She has released one EP titled Disconnect Me and three albums titled Eye of Providence, Five and Orphans with the Agonist.

In general, the higher the concentration of inhibitor, the more agonist activity will be lowered. IC50 value increases as agonist concentration increases. Furthermore, depending on the type of inhibition other factors may influence IC50 value; for ATP dependent enzymes IC50 value has an interdependency with concentration of ATP, especially so if inhibition is all of it competitive.

4a-Aryl- trans-decahydroisoquinolines. US Patent 4419517, Apr 8, 1975Henry Rapoport et al. Synthesis of 4A-aryl-decahydroisoquinolines. US Patent 4189583, Apr 26, 1978 Ciprefadol is a mixed agonist–antagonist at μ-opioid receptors and can partly block the effects of morphine at low doses, though at higher doses it acts more like a full agonist.

Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. Edited by David E. Golan. Lippincott Williams & Wilkins, 2011 . Page 308 In vitro studies have found that homotaurine is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy, becoming an antagonist and displacing the full agonists GABA and baclofen at this receptor.

To date, the Agonist has released six studio albums; the latest, Orphans, was released in September 2019.The Agonist To Release 'Five' Album In September - Blabbermouth.net Touring extensively since their first album, they have shared the stage with bands such as Arsonists Get All the Girls, Epica, the Faceless, Chelsea Grin, Kamelot, and Visions of Atlantis.

Clonidine is an alpha receptor agonist that helps reduces sympathetic activity leaving the hypothalamus and reduces circulating catecholamines. It is helpful in lowering blood pressure and heart rate, but it does not show much of an effect on other symptoms. It may also increase sympathetic inhibition in the brainstem. Bromocriptine is a dopamine agonist that helps lower blood pressure.

Dewick, pp. 374–375 So ergotamine is a partial agonist of α-adrenergic and 5-HT2 receptors, and thus narrows blood vessels and stimulates constriction of the uterus. Dihydroergotamine is more selective to α-adrenergic receptors and has a weaker effect on serotonin receptors. Ergometrine is an agonist of α-adrenergic, 5-HT2 and partly D2 receptors.

77-LH-28-1 is a selective agonist of muscarinic acetylcholine receptor subtype 1 (M1) discovered in 2008. It is an allosteric agonist, exhibiting over 100-fold specificity for M1 over other muscarinic receptor subtypes. 77-LH-28-1 penetrates the brain by crossing the blood-brain barrier and is therefore a useful pharmacological tool with cognition enhancing effects.

Etazocine (NIH-7856) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist of the opioid receptors, with mixed agonist and antagonist effects. In animal studies, it was shown to induce analgesia, dependency, and respiratory depression, with overall effects similar to those of morphine, but with substantially reduced potency in comparison.

It is unclear if use during pregnancy is safe and use while breastfeeding is not recommended. Buprenorphine affects different types of opioid receptors in different ways. Depending on the type of receptor it may be an agonist, partial agonist, or antagonist. Buprenorphine was patented in 1965 and approved for medical use in the United States in 1981.

Affinity for competitive agonists and antagonists is related by the Cheng-Prusoff factor used to calculate the Ki (affinity constant for an antagonist) from the shift in IC50 that occurs during competitive inhibition. The Cheng-Prusoff factor takes into account the effect of altering agonist concentration and agonist affinity for the receptor on inhibition produced by competitive antagonists.

Nalbuphine was first synthesized in 1965 and was introduced for medical use in the United States in 1979. In the search for opioid analgesics with less abuse potential than pure MOR agonist opioids, a number of semisynthetic opioids were developed. These substances are referred to as mixed agonist–antagonists analgesics. Nalbuphine belongs to this group of substances.

17α-OHP is an agonist of the progesterone receptor (PR) similarly to progesterone, albeit weakly in comparison. In addition, it is an antagonist of the mineralocorticoid receptor (MR) as well as a partial agonist of the glucocorticoid receptor (GR), albeit with very low potency (EC50 >100-fold less relative to cortisol) at the latter site, also similarly to progesterone.

Beta-2 agonist is a drug that opens the bronchial airways and often helps build muscle. Agonist is often referred to as a drug that stimulates natural processes in the body and beta-2 to a cell receptor. They are clinically used to help asthma patients. Yet, the abuse of beta-3 agonists can be used as an enhancer.

Trepipam (INN) is a dopamine receptor agonist of the benzazepine group that was never marketed. See also: AK-89719 [67287-53-0].

It has also been shown to function as a 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2B receptor antagonist.

Alnespirone (S-20,499) is a selective 5-HT1A receptor full agonist of the azapirone chemical class. It has antidepressant and anxiolytic effects.

Dinoxyline is a synthetic compound developed for scientific research, which acts as a potent full agonist at all five dopamine receptor subtypes.

Bazedoxifene is a selective estrogen receptor modulator (SERM), or a mixed agonist and antagonist of the estrogen receptor (ER) in different tissues.

FDU-PB-22 acts as a full agonist with a binding affinity of 1.19nM at CB1 and 2.43nM at CB2 cannabinoid receptors.

FUB-PB-22 acts as a full agonist with a binding affinity of 0.386nM at CB1 and 0.478nM at CB2 cannabinoid receptors.

GPER-selective ligands (that do not bind the classical estrogen receptors) include the agonist G-1 and the antagonists G15 and G36.

Impromidine (INN) is a highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.

Choline m-bromophenyl ether (MBF) is an extremely potent nicotinic agonist. It has powerful ganglion stimulating effects. It also causes muscle contractions.

MRS-1706 is a selective inverse agonist for the adenosine A2B receptor. It inhibits release of interleukins and has an antiinflammatory effect.

ALKS-5461 is a (1:1 ratio) combination of: (1) buprenorphine, a weak partial agonist of the μ-opioid receptor (MOR), antagonist/very weak partial agonist of the κ-opioid receptor (KOR), and, to a lesser extent, antagonist of the δ-opioid receptor (DOR) and weak partial agonist of the nociceptin receptor (NOP); and (2) samidorphan, a preferential antagonist of the MOR (but also, to a slightly lesser extent, weak partial agonist of the KOR and DOR).Almarsson, O., Deaver, D., Turncliff, R., Wentland, M., & Ehrich, E. (2010). Discovery and early development of ALKS-33, an opioid modulator for treatment of reward disorders. Abstracts Of Papers Of The American Chemical Society, 240 The combination of these two drugs putatively results in what is functionally a blockade of KORs with negligible activation of MORs.

EAM-2201 acts as a full agonist with a binding affinity of 0.380 nM at CB1 and 0.371 nM at CB2 cannabinoid receptors.

It is also a potent κ-opioid agonist, unlike the corresponding N-methyl and N-phenethyl derivatives which are reasonably μ-selective agonists.

8-OH-PBZI is a drug used in scientific research which acts as a potent and selective agonist for the dopamine D3 receptor.

2-OH-NPA is a drug used in scientific research which acts as a potent and selective agonist for the dopamine D2 receptor.

Dinapsoline is a drug developed for the treatment of Parkinson's disease, that acts as a selective full agonist at the dopamine D1 receptor.

FUB-APINACA acts as a full agonist with a binding affinity of 1.06 nM at CB1 and 0.174 nM at CB2 cannabinoid receptors.

ADBICA is a potent agonist of the CB1 receptor and CB2 receptor with an EC50 value of 0.69 nM and 1.8 nM respectively.

THJ-018 acts as a full agonist with a binding affinity of 5.84 nM at CB1 and 4.57 nM at CB2 cannabinoid receptors.

No non-peptide ligands for this receptor have yet been discovered, but as of 2009 both selective agonist and antagonist peptides are known.

FAUC50 is a covalent agonist of the β2 adrenoceptor. It has been used as a template to form covalent agonists for other receptors.

Alentemol (INN) (developmental code name U-66444B), or alentamol, is a selective dopamine autoreceptor agonist described as an antipsychotic, which was never marketed.

5F-APINACA acts as a full agonist with a binding affinity of 1.94 nM at CB1 and 0.266 nM at CB2 cannabinoid receptors.

Cortivazol is a high-affinity agonist ligand for the glucocorticoid receptor and consequently is classified as a glucocorticoid. It is sometimes abbreviated "CVZ".

Anabaseine causes paralysis in crustaceans and insects, but not in vertebrates, presumably by acting as an agonist on peripheral neuromuscular nicotinic acetylcholine receptors.

Certain MRAs interact with other presynaptic intracellular receptors which promote monoamine neurotransmission as well (e.g., methamphetamine is also an agonist at σ1 receptor).

A full agonist of VGSC site two, batrachotoxin, was then used to determine to what extent hoiamide A acted as an agonist. The experiments demonstrated that hoiamide A is a partial agonist because the maximum sodium influx hoiamide A binding caused was less than that of batrachotoxin. The chemical structure of hoiamide A and B Another study found that hoiamide A stimulated capspase-3 activity, lactic acid dehydrogenase efflux, and nuclear condensation. These processes are specifically and uniquely involved in necrosis and apoptosis, suggesting that hoiamide A is involved neuronal death by both necrosis and apoptosis.

Epiboxidine is a chemical compound which acts as a partial agonist at neural nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. It was developed as a less toxic analogue of the potent frog-derived alkaloid epibatidine, which is around 200 times stronger than morphine as an analgesic but produces extremely dangerous toxic nicotinic side effects. Epiboxidine is around one-tenth as potent as epibatidine as an α4β2 agonist, but has around the same potency as an α3β4 agonist. It has only one-tenth of the analgesic power of epibatidine, but is also much less toxic.

BML-190 (Indomethacin morpholinylamide) is a drug used in scientific research that acts as a selective CB2 inverse agonist. BML-190 is structurally derived from the NSAID indomethacin but has a quite different biological activity. The activity produced by this compound is disputed, with some sources referring to it as a CB2 agonist rather than an inverse agonist; this may reflect an error in classification, or alternatively it may produce different effects in different tissues, and more research is required to resolve this dispute. Lead optimization of the parent structure resulted in L-768,242 & L-759,787.

Electromyography (EMG) recordings of demonstrate the triphasic muscle activation begins with a brief agonist motor unit activation signal with firing rates of 60 to 120 Hz that may last for 100ms and occurs 50 to 100ms before movement begins. The firing rates of ballistic movements are much higher than that of slow ramp movements (5–15 Hz). The brief agonist muscle contraction is thus followed by antagonist muscle unit activation. The degree of antagonist muscle unit activation is dependent on the task at hand unlike the first agonist muscle activation which is independent to environmental stimuli.

The chemical structure of Solabegron, a β3-adrenergic receptor agonist Mirabegron is a selective β3-AR agonist that affects the detrusor muscles of the urinary bladder. By stimulation of β3-AR the contraction of the smooth muscles of the bladder is decreased and the bladder can store more volume of urine at a given time. Mirabegron also has an influence on the non-voiding contraction by decreasing the frequency of the contractions. The chemical structure of Vibegron, a β3-adrenergic receptor agonist In 2018 two other β3-AR agonists are in clinical trials, Vibegron and Solabegron.

A-412,997 is a drug which acts as a dopamine agonist that is used in scientific research. It is the first drug developed that is a highly selective agonist for the D4 subtype, with significantly improved selectivity over older D4-preferring compounds such as PD-168,077 and CP-226,269. In animal tests it improved cognitive performance in rats to a similar extent as methylphenidate, but without producing place preference or other signs of abuse liability. Also unlike other dopamine agonists, selective D4 agonists do not cause side effects such as sedation and nausea, and so might have advantages over older dopamine agonist drugs.

Talsaclidine (WAL-2014) is a non-selective muscarinic acetylcholine receptor agonist which acts as a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes. It was under development for the treatment of Alzheimer's disease but showed only modest or poor efficacy in rhesus monkeys and humans, respectively, perhaps due to an array of dose-limiting side effects including increased heart rate and blood pressure, increased salivation, urinary frequency and burning upon urination, increased lacrimation and nasal secretion, abnormal accommodation, heartburn, upset stomach as well as cramps, nausea, vomiting and diarrhea, excessive sweating and palpitations.

N-Methyl-D-aspartic acid (NMDA), a synthetic partial agonist of the main site of the NMDAR. N-Methyl-D-aspartic acid (NMDA), which the NMDA receptor was named after, is a partial agonist of the active or glutamate recognition site. 3,5-Dibromo-L-phenylalanine, a naturally occurring halogenated derivative of L-phenylalanine, is a weak partial NMDA receptor agonist acting on the glycine site. 3,5-Dibromo-L-phenylalanine has been proposed a novel therapeutic drug candidate for treatment of neuropsychiatric disorders and diseases such as schizophrenia, and neurological disorders such as ischemic stroke and epileptic seizures.

The level of activity of the receptor will be determined by the relative affinity of each molecule for the site and their relative concentrations. High concentrations of a competitive agonist will increase the proportion of receptors that the agonist occupies, higher concentrations of the antagonist will be required to obtain the same degree of binding site occupancy. In functional assays using competitive antagonists, a parallel rightward shift of agonist dose–response curves with no alteration of the maximal response is observed. Competitive antagonists are used to prevent the activity of drugs, and to reverse the effects of drugs that have already been consumed.

Goserelin, sold under the brand name Zoladex among others, is a medication which is used to suppress production of the sex hormones (testosterone and estrogen), particularly in the treatment of breast and prostate cancer. It is an injectable gonadotropin releasing hormone agonist (GnRH agonist). Structurally, it is a decapeptide. It is the natural GnRH decapeptide with two substitutions to inhibit rapid degradation.

A fifth endocannabinoid, virodhamine, or O-arachidonoyl-ethanolamine (OAE), was discovered in June 2002. Although it is a full agonist at CB2 and a partial agonist at CB1, it behaves as a CB1 antagonist in vivo. In rats, virodhamine was found to be present at comparable or slightly lower concentrations than anandamide in the brain, but 2- to 9-fold higher concentrations peripherally.

Magnolol is also binding in dimeric mode to PPARγ, acting as an agonist of this nuclear receptor.Dreier D, Latkolik S, Rycek L, Schnürch M, Dymáková A, Atanasov AG, Ladurner A, Heiss EH, Stuppner H, Schuster D, Mihovilovic MD, Dirsch VM. Linked magnolol dimer as a selective PPARγ agonist - Structure- based rational design, synthesis, and bioactivity evaluation. Sci Rep. 2017 Oct 20;7(1):13002.

Betahistine is a strong antagonist of the histamine H3 receptor and a weak agonist of the histamine H1 receptor. Betahistine has two mechanisms of action. Primarily, it is a weak agonist on the H1 receptors located on blood vessels in the inner ear. This gives rise to local vasodilation and increased permeability, which helps to reverse the underlying problem of endolymphatic hydrops.

However, with regular beta-2 agonist use, asthmatic Arg-16 individuals experience a significant decline in bronchodilator response. This decline does not occur in Gly-16 individuals. It has been proposed that the tachyphylactic effect of regular exposure to exogenous beta-2 agonists is more apparent in Arg-16 individuals because their receptors have not been downregulated prior to agonist administration.

The flaw in Clark's receptor-occupancy model was that it was insufficient to explain the concept of a partial agonist. This led to the development of agonist models of drug action by Ariens in 1954 and by Stephenson in 1956 to account for the intrinsic activity (efficacy) of a drug (that is, its ability to induce an effect after binding).

Common side effects include low blood sugar, nausea, dizziness, abdominal pain, and pain at the site of injection. Other serious side effects may include medullary thyroid cancer, angioedema, pancreatitis, gallbladder disease, and kidney problems. Use in pregnancy and breastfeeding is of unclear safety. Liraglutide is a glucagon-like peptide-1 receptor agonist (GLP-1 receptor agonist) also known as incretin mimetics.

Moxazocine (BL-4566) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist or mixed agonist/antagonist of the opioid receptors and binds preferentially to the κ-opioid receptor. Despite its failure to reach the market, clinical studies demonstrated moxazocine to be approximately 10x as potent by weight as morphine as an analgesic.

AMG-36 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is a derivative of Δ8THC substituted with a cyclopentane group on the 3-position side chain. AMG-36 is a potent agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 0.45 nM at CB1 vs 1.92 nM at CB2.

AMG-1 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is a derivative of Δ8THC with a rigidified and extended 3-position side chain. AMG-1 is a potent agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 0.6 nM at CB1 vs 3.1 nM at CB2.

AMG-41 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is a derivative of Δ8-THC substituted with a cyclopropyl group on the C1'-position of the C3-alkyl side chain. AMG-41 is a potent agonist at both CB1 and CB2, with a Ki of 0.44 nM at CB1 vs 0.86 nM at CB2.

1-Amino-1,3-dicarboxycyclopentane (ACPD) is a chemical compound that binds to the metabotropic glutamate receptor (mGluR), acting as a mGluR agonist. ACPD is a rigid analogue of the neurotransmitter glutamate and does not activate ionotropic glutamate receptors. However, it has been reported to be an agonist of the glycine site of the NMDA receptor. ACPD can induce convulsions in neonatal rats.

Pitolisant is an H3-receptor inverse agonist. As H3 receptors mainly act as autoreceptors, pitolisant decreases negative feedback to histaminergic neurons, enhancing histaminergic transmission.

These findings were mimicked by another, structurally different CB2 agonist, GW-405,833, and were reversed by the administration of a CB2 antagonist, AM-630.

Like the other fibrates, bezafibrate is an agonist of PPARα; some studies suggest it may have some activity on PPARγ and PPARδ as well.

5-Benzyloxytryptamine (5-BT), is a tryptamine derivative which acts as an agonist at the 5-HT1D, 5-HT2 and 5-HT6 serotonin receptors.

5F-PB-22 acts as a full agonist with a binding affinity of 0.468 nM at CB1 and 0.633 nM at CB2 cannabinoid receptors.

In human breast cancer cell lines, quercetin has also been found to act as an agonist of the G protein-coupled estrogen receptor (GPER).

Alternariol product page from Fermentek It is also a mycoestrogen. Alternariol is reported to be a full androgen agonist in an in vitro assay.

Pregnenolone has been found to act as an agonist of the pregnane X receptor. Pregnenolone has no progestogenic, corticosteroid, estrogenic, androgenic, or antiandrogenic activity.

Flutamide has been identified as an agonist of the aryl hydrocarbon receptor. This may be involved in or responsible for the hepatotoxicity of flutamide.

Five is the fifth studio album and Napalm Records debut by Canadian metal band the Agonist. The album was released on September 30, 2016.

In general, a primary or secondary aliphatic amine separated by 2 carbons from a substituted benzene ring is minimally required for high agonist activity.

Chirally active tryptophan by Larock indole synthesis Other relevant applications include the synthesis of 5-HT1D receptor agonist MK-0462, an anti-migraine drug.

On the other hand, agonist activity is also shown in ligands with larger groups at the morphinan nitrogen, and therefore this hypothesis is challenged.

To induce unconsciousness, anesthetics affect the GABA and NMDA systems. For example, propofol is a GABA agonist, and ketamine is an NMDA receptor antagonist.

Melina has been collaborating with several other established musicians such as singer-songwriter guitarist Sule Heitner, electronica producer Override and metal band The Agonist.

Deoxyschizandrin is a bio-active isolate of Schisandra chinensis. Deoxyschizandrin has been found to act as an agonist of the adiponectin receptor 2 (AdipoR2).

7-Spiroindanyloxymorphone (SIOM) is a drug that is used in scientific research. It is a selective δ-opioid agonist. It is a derivative of oxymorphone.

For instance, it is 40-fold less potent in promoting internalization (receptor downregulation) of the human KOR relative to the prototypical KOR agonist U-50488.

Ro10-5824 is a drug which acts as a dopamine receptor partial agonist selective for the D4 subtype, and has nootropic effects in animal studies.

MK-212 (CPP or 6-chloro-2-(l-piperazinyl)pyrazine) is a serotonin agonist. It promotes the secretion of serum prolactin and cortisol in humans.

Methacholine (INN, USAN) (trade name Provocholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.

A-40174 (SP-1) is an analgesic drug which acts as a potent cannabinoid receptor agonist, and was developed by Abbott Laboratories in the 1970s.

6'-Guanidinonaltrindole (6'-GNTI) is a κ−δ-opioid receptor selective ligand used in scientific research. With 6'-GNTI, evidence was provided for the first time that receptor oligomerization plays functional role in living organisms. 6'-GNTI is an extremely biased agonist of the κ-opioid receptor. It is a potent partial agonist of the G protein pathway but does not recruit the β-arrestin pathway.

Formoterol, another long-acting β2-agonist, was marketed shortly after. This long duration of action made the treatment for severe asthma and COPD more convenient for the patients because it is inhaled twice a day. In 2013 an extra long-acting β2-agonist, vilanterol, was marketed. Its duration of action lasts for 24 hours which should improve patients' compliance and make the treatment more convenient.

Surgical removal is the usual treatment for GH-producing tumors. In some circumstances, focused radiation or a GH antagonist such as pegvisomant may be employed to shrink the tumor or block function. Other drugs like octreotide (somatostatin agonist) and bromocriptine (dopamine agonist) can be used to block GH secretion because both somatostatin and dopamine negatively inhibit GHRH-mediated GH release from the anterior pituitary.

Expression of the GABABR2 subunit alone, meanwhile, leads to surface expression of the subunit, although with no functional activity (i.e., the receptor does not bind agonist and cannot initiate a response following exposure to agonist). Expression of the two subunits together leads to plasma membrane expression of functional receptor. It has been shown that GABABR2 binding to GABABR1 causes masking of a retention signal of functional receptors.

Three-tiered hierarchy of the muscle synergy hypothesis with m synergies and n effector muscles. A muscle synergy is a group of synergistic muscles and agonists that work together to perform a motor task. A muscle synergy is composed of agonist and synergistic muscles. An agonist muscle is a muscle that contracts individually, and it can cause a cascade of motion in neighboring muscles.

Prucalopride, a first in class benzofuran, is a selective, high affinity serotonin (5-HT4) receptor agonist that stimulates colonic mass movements, which provide the main propulsive force to defecation.SmPC. Summary of product characteristics Resolor (prucalopride)October, 2009:1-9.Bouras EP, Camilleri M, Burton DD, McKinzie S. Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans. Gut. May 1999;44(5):682-686.

Amibegron (SR-58,611A) was a drug developed by Sanofi-Aventis (now Sanofi) which acts as a selective agonist for the β3 adrenergic receptor. It is the first orally active β3 agonist developed that is capable of entering the central nervous system, and has antidepressant and anxiolytic effects. On July 31, 2008, Sanofi-Aventis announced that it has decided to discontinue development of amibegron.Second quarter 2008 results.

Effects of the competitive inhibition of an agonist by increases in the concentration of an antagonist. A drugs potency can be affected (the response curve shifted to the right) by the presence of an antagonistic interaction.pA2 known as the Schild representation, a mathematical model of the agonist:antagonist relationship or vice versa. NB: the x-axis is incorrectly labelled and should reflect the agonist concentration, not antagonist concentration.

Although cabergoline is commonly described principally as a dopamine D2 receptor agonist, it also possesses significant affinity for the D3, D4, 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, α2B\- receptors, and moderate/low affinity for the D1 and 5-HT7 receptors. Cabergoline functions as an agonist at all of these receptors except for 5-HT7 and α2B-, where it acts as an antagonist.

Sazetidine A (AMOP-H-OH) is a drug which acts as a subtype selective partial agonist at α4β2 neural nicotinic acetylcholine receptors, acting as an agonist at (α4)2(β2)3 pentamers, but as an antagonist at (α4)3(β2)2 pentamers. It has potent analgesic effects in animal studies comparable to those of epibatidine, but with less toxicity, and also has antidepressant action.

In 1984 the β3 receptor was described as the third group of beta receptors in adipose tissue. This led to the development of agonist targeted at obesity and diabetes. In 1999 the function of the β3 in detrusor muscles was defined which opened the way for development of β3-AR agonist for OAB. In 2001 Mirabegron began clinical development in phase 1 clinical study.

The most common of these binding sites, benzodiazepine, allows for both agonist and antagonist effects on the receptor. A common drug, diazepam, acts as an allosteric enhancer at this binding site. Another receptor for GABA, known as GABAB, can be enhanced by a molecule called baclofen. This molecule acts as an agonist, therefore activating the receptor, and is known to help control and decrease spastic movement.

Estradiol is an estrogen, or an agonist of the estrogen receptors (ERs), the and . It is also an agonist of membrane estrogen receptors (mERs), including the , , ER-X, and ERx. Estradiol is highly selective for these ERs and mERs, and does not interact importantly with other steroid hormone receptors. It is far more potent as an estrogen than are other bioidentical estrogens like estrone and estriol.

Agonist muscles and antagonist muscles refer to muscles that cause or inhibit a movement. Agonist muscles cause a movement to occur through their own activation. For example, the triceps brachii contracts, producing a shortening contraction, during the up phase of a push-up (elbow extension). During the down phase of a push-up, the same triceps brachii actively controls elbow flexion while producing a lengthening contraction.

Zucapsaicin excites and desensitizes C-fibers via agonist at TRPV1 on nociceptive neurons. It binds to intracellular sites and initially stimulates the channels, causing burning sensation. The mechanism of pharmacological action of zucapsaicin has not been fully understood yet. It is suggested that this compound, similarly to its trans isomer, is an agonist of the vanilloid receptor VR1 (TRPV1) and a neuronal calcium channel blocker.

Tetryzoline is an alpha agonist for alpha-2 receptor and imidazoline receptor I-1 agonist. Mainly due to its alpha-2 agonism it can constrict conjuctival blood vessels of the eye when taken in the form of eye drops. This relieves the redness of the eye caused by minor ocular irritants. To treat allergic conjunctivitis, tetryzoline can be combined in a solution with antazoline.

Albiglutide (trade names Eperzan in Europe and Tanzeum in the US) is a glucagon-like peptide-1 agonist (GLP-1 agonist) drug marketed by GlaxoSmithKline (GSK) for treatment of type 2 diabetes. As of 2017 it is unclear if it affects a person's risk of death. GSK has announced that it intends to withdraw the drug from the worldwide market by July 2018 for economic reasons.

As such, due to its high affinity for the σ1 receptor, (+)-alazocine can be used to distinguish between the two sigma receptor subtypes in scientific research, for instance in radioligand binding assays. Taken together, (–)-alazocine is a selective partial agonist of the κ-opioid receptor, antagonist of the μ-opioid receptor, and to a far lesser extent agonist of the δ-opioid receptor with very low affinity for the sigma receptors, while (+)-alazocine is a selective agonist of the sigma σ1 receptor and to a lesser (~10-fold) extent antagonist of the NMDA receptor with low affinity for the opioid and sigma σ2 receptors.

In 2014, tianeptine was found to be a μ-opioid receptor (MOR) full agonist using human proteins. It was also found to act as a full agonist of the δ-opioid receptor (DOR), although with approximately 200-fold lower potency. The same researchers subsequently found that the MOR is required for the acute and chronic antidepressant-like behavioral effects of tianeptine in mice and that its primary metabolite had similar activity as a MOR agonist but with a much longer elimination half-life. Moreover, although tianeptine produced other opioid-like behavioral effects such as analgesia and reward, it did not result in tolerance or withdrawal.

SL651498 is a subtype-selective GABAA agonist, which acts as a full agonist at α2 and α3 subtypes, and as a partial agonist at α1 and α5 (although its action at α5 subtypes is much weaker than at the others). In animal studies, it has primarily anxiolytic effects, although some sedation, ataxia and muscle relaxant effects are observed at higher doses. It substitutes fully for the anxiolytic benzodiazepine chlordiazepoxide, but only partially substituted for the imidazopyridine hypnotic drug zolpidem and the benzodiazepine hypnotic triazolam. When given repeatedly it failed to produce tolerance or dependence, probably due to its low affinity and efficacy at the α5 subtype.

Saralasin is a partial agonist of angiotensin II receptors, though it is commonly mistaken as a competitive antagonist. Saralasin's distinction as a partial agonist is based on the fact that its therapeutic effect (i.e. reduced hypertension) is only observed in patients with high plasma angiotensin II levels, but in patients with low angiotensin II levels saralasin causes hypertension. In other words, the effects of saralasin on the angiotensin II receptor in the absence of angiotensin II is pharmacodynamically similar to angiotensin II itself thus it is a partial agonist, because if it was an antagonist it would not elicit an effect when bound to its receptor.

Mitragynine acts on a variety of receptors in the CNS, most notably the mu, delta, and kappa opioid receptors. The nature of mitragynines' interaction with opioid receptors has yet to be fully classified with some reports suggesting partial agonist activity at the mu opioid receptor and others suggesting full agonist activity. Additionally, mitragynine is known to interact with delta and kappa opioid receptors as well, but these interactions remain ambiguous with some reports indicated mitragynine as a delta and kappa competitive antagonist and others as a full agonist of these receptors. In either case, mitragynine is reported to have lower affinity to delta and kappa receptors compared to mu receptors.

This property earns them the name "non-competitive" because their effects cannot be negated, no matter how much agonist is present. In functional assays of non-competitive antagonists, depression (physiology) of the maximal response of agonist dose-response curves, and in some cases, rightward shifts, is produced. The rightward shift will occur as a result of a receptor reserve (also known as spare receptors) and inhibition of the agonist response will only occur when this reserve is depleted. An antagonist that binds to the active site of a receptor is said to be "non-competitive" if the bond between the active site and the antagonist is irreversible or nearly so.

Nebracetam is an investigational drug of the racetam family that is a M1 acetylcholine receptor agonist in rats. Its effects in humans have not been studied.

Norgesterone is a progestogen, and hence is an agonist of the progesterone receptor. Unlike related progestins, it is virtually devoid of androgenic activity in animal assays.

Homocysteic acid is a sulfur-containing glutamic acid analog and a potent NMDA receptor agonist. It is related to homocysteine, a by-product of methionine metabolism.

The behavior of each of these receptors under prolonged exposure to their chief agonist - melatonin - is indicative of the functions that they are each crucial to.

Naboctate (SP-325) is a synthetic cannabinoid receptor agonist, which has antiemetic, sedative, anxiolytic and anti-glaucoma properties.Concise dictionary of pharmacological agents: properties and synonyms. p188.

Reproterol is a short-acting β2 adrenoreceptor agonist used in the treatment of asthma. It was patented in 1965 and came into medical use in 1977.

Misoprostol is an agonist of EP1 and EP3 receptors, and can cause a greater stimulation at lower concentrations. At higher concentrations, the medication can suppress contractions.

3D structure of paricalcitol Like 1,25-dihydroxyergocalciferol, paricalcitol acts as an agonist at the vitamin D receptor and thereby lowers parathyroid hormone levels in the blood.

SR-57227 is a potent and selective agonist at the 5HT3 receptor, with high selectivity over other serotonin receptor subtypes and good blood-brain barrier penetration.

CID16020046 is a compound which acts as an inverse agonist at the former orphan receptor GPR55, and may be the first selective inverse agonist characterised for this receptor. It was found to block a number of GPR55 mediated responses such as wound healing and activation of immune system T-cells and B-cells, as well as showing inverse agonist activity in the absence of GPR55 agonist stimulation. However while it was found to have good selectivity over the related CB1 and CB2 cannabinoid receptors as well as a number of other targets, CID16020046 has not yet been tested against another related receptor GPR18, so its selectivity for GPR55 over this target has not been established. It has antiinflammatory actions, has been used to study the interaction between GPR55 mediated and CB1 mediated activity, and research using this compound has revealed a role for GPR55 in learning and memory.

Also the last album with singer Angela Gossow before she stepped down as vocalist in March, 2014 to be succeeded by the Agonist singer Alissa White-Gluz.

The same cardiomyocytes also increase their firing rate with agonist exposure under a current-clamp tetanus protocol suggesting that they may play a role in cardiac arrhythmogenesis.

The smaller the EC50 value, the greater the potency of the agonist, the lower the concentration of drug that is required to elicit the maximum biological response.

Similarly, in a series of case studies, delusions of guilt and punishment were found in Austrian patients with Parkinson's being treated with l-dopa, a dopamine agonist.

Testosterone cypionate is a prodrug of testosterone and is an androgen and anabolic–androgenic steroid (AAS). That is, it is an agonist of the androgen receptor (AR).

Testosterone enanthate is a prodrug of testosterone and is an androgen and anabolic–androgenic steroid (AAS). That is, it is an agonist of the androgen receptor (AR).

Testosterone propionate is a prodrug of testosterone and is an androgen and anabolic–androgenic steroid (AAS). That is, it is an agonist of the androgen receptor (AR).

Recently, a close derivative of 5-CT, AH-494 has been shown to function as an agonist of 5-HT7, although being more selective over 5-HT1A.

SKF-38,393 is a synthetic compound of the benzazepine chemical class which acts as a selective D1/D5 receptor partial agonist. It has stimulant and anorectic effects.

Testosterone undecanoate is a prodrug of testosterone and is an androgen and anabolic–androgenic steroid (AAS). That is, it is an agonist of the androgen receptor (AR).

Eglumegad acts as a group- selective agonist for the group II metabotropic glutamate receptors (mGluR2/3). It is unclear whether eglumegad directly interacts with dopamine D2 receptors.

It has been demonstrated that deletion and overexpression of PDE1 produces strong effects on agonist-induced cAMP signalling but has little effect on the basal cAMP level.

As with all ligand-gated ion channels, opening of the nAChR channel pore requires the binding of a chemical messenger. Several different terms are used to refer to the molecules that bind receptors, such as ligand, agonist, or transmitter. As well as the endogenous agonist acetylcholine, agonists of the nAChR include nicotine, epibatidine, and choline. Nicotinic antagonists that block the receptor include mecamylamine, dihydro-β-erythroidine, and hexamethonium.

Histrelin acetate, sold under the brand names Vantas and Supprelin LA among others, is a nonapeptide analogue of gonadotropin-releasing hormone (GnRH) with added potency.Histrelin acetate (Vantas) - New Drug Bulletins When present in the bloodstream, it acts on particular cells of the pituitary gland called gonadotropes. Histrelin stimulates these cells to release luteinizing hormone and follicle-stimulating hormone. Thus it is considered a gonadotropin-releasing hormone agonist or GnRH agonist.

L-759,633 is an analgesic drug that is a cannabinoid agonist. It is a fairly selective agonist for the CB2 receptor, with selectivity of 163x for CB2 over CB1. It produces some similar effects to other cannabinoid agonists such as analgesia, but with little or no sedative or psychoactive effects due to its weak CB1 activity, and a relatively strong antiinflammatory effect due to its strong activity at CB2.

In the example, the door is the agonist and the force preventing the door from being opened is the Antagonist. Force entities have an intrinsic force tendency, either toward action or toward rest. For the agonist, this tendency is marked with an arrowhead (action) or with a large dot (rest) (see b, figure 1). Since the antagonist by definition has an opposing tendency, it need not be marked.

2,3-Dichlorophenylpiperazine (2,3-DCPP or DCPP) is a chemical compound from the phenylpiperazine family. It is both a precursor in the synthesis of aripiprazole and one of its metabolites. It is unclear whether 2,3-DCPP is pharmacologically active as a serotonin receptor agonist similar to its close analogue 3-chlorophenylpiperazine (mCPP), though it has been shown to act as a partial agonist of the dopamine D2 and D3 receptors.

6-Fluoronorepinephrine (6-FNE) is a selective α1 and α2 adrenergic receptor full agonist related to norepinephrine. It is the only selective full agonist for the α adrenergic receptors known to date and has been used to study their function in scientific research. Infusion of 6-FNE into the locus coeruleus of rodents produces marked hyperactivity and behavioral disinhibition by suppressing activity in the area via stimulation of α1 adrenergic receptors.

The KOR agonist salvinorin-A, for example, causes an overall decrease in ICSS response rates at lower stimulation frequencies. Repeated administration does not produce tolerance to ICSS depression. The effects of delta opioid receptor (DOR) agonists/antagonists on ICSS are less clear. One DOR agonist, SNC80, has been found to cause ICSS depression, but there is counter-evidence suggesting some delta agonists might have weak ICSS facilitation properties.

One alternative is to use a GnRH agonist instead of hCG. While this has been repeatedly shown to "virtually eliminate" OHSS risk, there is some controversy regarding the effect on pregnancy rates if a fresh non-donor embryo transfer is attempted, almost certainly due to a luteal phase defect. There is no dispute that the GnRH agonist trigger is effective for oocyte donors and for embryo banking (cryopreservation) cycles.

When screening mutants selection will be for thermal stability in the specific conformation, i.e., if the radioligand is an agonist, selection will be for the agonist binding conformation and if it is an antagonist, then the screening is for stability in the antagonist binding conformation. Radioassays have the advantage of working with minute amounts of protein. But it is work with radioactive substances and large amount of manual labour is involved.

This effect explains the euphoria experienced by ingestion of this "agonist." Initially, hallucinogens were thought to blockade these serotonin neurotransmitters, but persistent research led to this agonist effect conclusion. Woolley and Campbell conducted research to determine whether the depletion of the hormone serotonin had a direct effect on mental disorders and that hallucinations might be due to an excess of serotonin. Their results led them to study chemicals analogous to serotonin.

Gamma-aminobutyric acid. A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. There are three receptors of the gamma-aminobutyric acid. The two receptors GABA-α and GABA-ρ are ion channels that are permeable to chloride ions which reduces neuronal excitability.

Exenatide is a glucagon-like peptide-1 receptor agonist (GLP-1 receptor agonist) also known as incretin mimetics. It works by increasing insulin release from the pancreas and decreases excessive glucagon release. Exenatide was approved for medical use in the United States in 2005. A month supply in the United Kingdom costs the NHS about £82 for the daily injectable and £73 for the weekly injectable version as of 2019.

AM-087 (part of the AM cannabinoid series) is an analgesic drug which acts as a cannabinoid agonist. It is a derivative of Δ8-THC, substituted on the 3-position side chain. AM-087 is a potent CB1 agonist with a Ki of 0.43 nM, making it around 100 times more potent than THC itself. This is most likely due to the bulky bromine substituent on the side chain.

In animal experiments, σ–antagonists such as rimcazole were able to block convulsions from cocaine overdose. σ–antagonists are also under investigation for use as antipsychotic medications. The abundant neurosteroid steroid hormone DHEA is an agonist at sigma receptors and along with pregnenolone could be endogenous agonist ligands; opposed by sigma antagonistic activity from progesterone. Another endogenous ligand, N,N-dimethyltryptamine, was also found to interact with σ1.

AM-905 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is conformationally restricted by virtue of the double bond on its side chain, leading an increased affinity for and selectivity between CB1 and CB2 receptors. It is a potent and reasonably selective agonist for the CB1 cannabinoid receptor, with a Ki of 1.2 nM at CB1 and 5.3 nM at CB2.

This avails for scheduling the egg retrieval procedure at a time where the eggs are fully mature. HCG injection confers a risk of ovarian hyperstimulation syndrome. Using a GnRH agonist instead of hCG eliminates most of the risk of ovarian hyperstimulation syndrome, but with a reduced delivery rate if the embryos are transferred fresh. For this reason, many centers will freeze all oocytes or embryos following agonist trigger.

For instance, an agonist will stabilize the active form of a pharmacological receptor. Phenomenologically, it looks as if the agonist provokes the conformational transition. One crucial feature of the model is the dissociation between the binding function (the fraction of protein bound to the regulator), and the state function (the fraction of protein under the activated state), cf below. In the models said of "induced-fit", those functions are identical.

Unlike ephedrine and tyramine, etafedrine does not induce the release of epinephrine or norepinephrine and instead acts as a selective β2 adrenoreceptor agonist, thereby mediating its bronchodilator effects.

This is suspected to be a result of the structural similarities between NAG and carabamoyl glutamate, which allows carbamoyl glutamate to act as an effective agonist for CPS1.

Isolated from the hallucinogenic sage Salvia divinorum, Salvinorin A is a potent and selective κ-opioid agonist. The compound has potential uses in psychotherapuetic treatments and Alzheimer's treatment.

ADB-FUBICA is a drug that acts as a potent agonist for the cannabinoid receptors, with EC50 values of 2.6 nM at CB1 and 3.0 nM at CB2.

AB-FUBICA is a drug that acts as a potent agonist for the cannabinoid receptors, with EC50 values of 21 nM at CB1 and 15 nM at CB2.

Colterol is a short-acting β2-adrenoreceptor agonist. Bitolterol, a prodrug for colterol, is used in the management of bronchospasm in asthma and chronic obstructive pulmonary disease (COPD).

FUB-PB-22 (QUFUBIC) is an indole-based synthetic cannabinoid that is a potent agonist of the CB1 receptor and has been sold online as a designer drug.

Galnon is a drug which acts as a selective, non-peptide agonist at the galanin receptors GALR. It has anticonvulsant, anxiolytic, anorectic and amnestic effects in animal studies.

25G-NBOMe (NBOMe-2C-G) is a derivative of the phenethylamine hallucinogen 2C-G, which acts as a highly potent partial agonist for the human 5-HT2A receptor.

DOC acts as a selective 5-HT2A, 5-HT2B, and 5-HT2C receptor partial agonist. Its psychedelic effects are mediated via its actions on the 5-HT2A receptor.

AM-1235 (1-(5-fluoropentyl)-3-(naphthalen-1-oyl)-6-nitroindole) is a drug that acts as a potent and reasonably selective agonist for the cannabinoid receptor CB1.

Nicotine acts as a receptor agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits (nAChRα9 and nAChRα10) where it acts as a receptor antagonist.

Trimbow is indicated for the maintenance treatment in adults with moderate to severe chronic obstructive pulmonary disease (COPD) who are not adequately treated by a combination of an inhaled corticosteroid and a long-acting beta2-agonist or a combination of a long- acting beta2-agonist and a long-acting muscarinic antagonist. Trydonis and Riarify are indicated for the maintenance treatment in adults with moderate to severe chronic obstructive pulmonary disease (COPD) who are not adequately treated by a combination of an inhaled corticosteroid and a long-acting beta2-agonist. Beclometasone belongs to a group of anti-inflammatory medicines known as corticosteroids. It works in a similar way to naturally occurring corticosteroid hormones, reducing the activity of the immune system.

Nalorphine () (brand names Lethidrone, Nalline), also known as N-allylnormorphine, is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence. It acts at two opioid receptors — the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (Ki = 1.6 nM; EC50 = 483 nM; Emax = 95%) where it exerts high-efficacy partial agonist/near-full agonist characteristics. Nalorphine was the second opioid antagonist to be introduced, preceded by nalodeine (N-allylnorcodeine) in 1915 and followed by naloxone in 1960 and naltrexone in 1963.

LY-379,268 is a drug that is used in neuroscience research, which acts as a potent and selective agonist for the group II metabotropic glutamate receptors (mGluR2/3). It is derived from the older mGluR group II agonist eglumegad, and led on to the development of the more potent compound LY-404,039, but is still widely used in research itself. LY-379,268 has sedative, neuroprotective, anti-addictive and anticonvulsant effects in animals, and blocks the effects of PCP and DOI, which has led to research into LY-379,268 and similar compounds as antipsychotic drugs for the treatment of schizophrenia in animals. There are inconsistent findings about an additional activity as a dopamine D2 receptor partial agonist.

If available, meptazinol, an opioid analgesic of the mixed agonist/antagonist type, should be administered to reduce the severity of the reaction. Anti TNF-a may also be effective.

Direct stimulation of the α- and β-adrenergic receptors can produce sympathomimetic effects. Salbutamol is a widely used direct-acting β2-agonist. Other examples include phenylephrine, isoproterenol, and dobutamine.

Befiradol (F-13,640; NLX-112) is an experimental drug being studied for the treatment of levodopa-induced dyskinesia. It is a potent and selective 5-HT1A receptor full agonist.

In addition to acting as an agonist there is evidence to show that ODAP is transported into the cell by an antiporter that simultaneously transports glutamate into the synapse.

These effects were completely inhibited by a selective 5-HT2C receptor antagonist, SB-242,084. Therefore, results suggest that YM348 is a potent and orally active 5-HT2C receptor agonist.

CP-226,269 is a drug which acts as a dopamine agonist selective for the D4 subtype, which is used for researching the role of D4 receptors in the brain.

The administration of the racemate results in the overall β1 agonism responsible for its activity. (+)-Dobutamine also has mild β2 agonist activity, which makes it useful as a vasodilator.

Eptazocine (Sedapain) is an opioid analgesic which was introduced in Japan by Morishita in 1987. It acts as a mixed κ-opioid receptor agonist and μ-opioid receptor antagonist.

Muscarine A muscarinic agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation.

Dextropropoxyphene acts as a mu-opioid receptor agonist. It also acts as a potent, noncompetitive α3β4 neuronal nicotinic acetylcholine receptor antagonist, as well as a weak serotonin reuptake inhibitor.

It was then discovered that the blockage of the CB1 receptor represented a new pharmacological target. The first specific CB1 receptor antagonist / inverse agonist was rimonabant, discovered in 1994.

Avitriptan (INN) (code name BMS-180,048) is an antimigraine drug of the triptan family which was never marketed. It acts as a 5-HT1B and 5-HT1D receptor agonist.

In comparison, β-phenethylamine itself had an ED50 of ~106 nM, with an Emax of ~ 100%. "Table 3" In other words, phenylethanolamine is a TAAR1 agonist and trace amine.

Binding affinity data alone does not determine the overall potency of a drug. Potency is a result of the complex interplay of both the binding affinity and the ligand efficacy. Ligand efficacy refers to the ability of the ligand to produce a biological response upon binding to the target receptor and the quantitative magnitude of this response. This response may be as an agonist, antagonist, or inverse agonist, depending on the physiological response produced.

It is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. GLP-1 is a hormone that is involved in the normalization of level of glucose in blood (glycemia). The Food and Drug Administration (FDA) approved dulaglutide for use in the United States in September 2014. It was approved for use in the European Union in November 2014.

Paracetamol (called acetaminophen in the US and Canada) is metabolically combined with arachidonic acid by FAAH to form AM404. This metabolite of paracetamol is a potent agonist at the TRPV1 vanilloid receptor, a weak agonist at both CB1 and CB2 receptors, and an inhibitor of anandamide reuptake. As a result, anandamide levels in the body and brain are elevated. In this fashion, paracetamol acts as a pro-drug for a cannabimimetic metabolite.

GHB has at least two distinct binding sites in the central nervous system. GHB is an agonist at the newly characterized GHB receptor, which is excitatory, and it is a weak agonist at the GABAB receptor, which is inhibitory. GHB is a naturally occurring substance that acts in a similar fashion to some neurotransmitters in the mammalian brain. GHB is probably synthesized from GABA in GABAergic neurons, and released when the neurons fire.

Talipexole (B-HT920, Domnin) is a dopamine agonist that is marketed as a treatment for Parkinson's Disease in Japan by Boehringer Ingelheim; it was introduced in 1996.PharmaLetter 22 July 1996 First Launch In Japan For Talipexole As of December 2014 it was not approved for marketing in the US nor in Europe.EvaluatePharma Database. Page accessed 9 December 2014 Talipexole is a D2 dopamine receptor agonist and interacts both pre- and post-synaptic receptors.

For example, when synergy occurs at a cellular receptor level this is termed agonism, and the substances involved are termed agonists. On the other hand, in the case of antagonism, the substances involved are known as inverse agonists. The different responses of a receptor to the action of a drug has resulted in a number of classifications, such as "partial agonist", "competitive agonist" etc. These concepts have fundamental applications in the pharmacodynamics of these interactions.

Meptazinol (trade name Meptid) is an opioid analgesic developed by Wyeth in the 1970s. Indications for use in moderate to severe pain, most commonly used to treat pain in obstetrics (childbirth). Meptazinol is a 3-phenylazepane derivative, whereas the other phenazepanes like ethoheptazine and proheptazine are 4-phenylazepanes. A partial μ-opioid receptor agonist, its mixed agonist/antagonist activity affords it a lower risk of dependence and abuse than full μ agonists like morphine.

Cirazoline is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α2 adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent. Cirazoline has also been shown to decrease food intake in rats, purportedly through activation of α1 adrenoceptors in the paraventricular nucleus in the hypothalamus of the brain.

Clenbuterol is approved for use in some countries as a bronchodilator for asthma. Clenbuterol is a β2 agonist with some structural and pharmacological similarities to epinephrine and salbutamol, but its effects are more potent and longer-lasting as a stimulant and thermogenic drug. It is commonly used for smooth muscle-relaxant properties as a bronchodilator and tocolytic. It is classified by the World Anti-Doping Association as an anabolic agent, not as a β2 agonist.

The proposed molecular mode of action of TRPV1 antagonists is blocking of the channel pore. Several studies using either capsaicin, pH values < 6 or heat as the agonist have shown that I-RTX works as a strong competitive TRPV1 antagonist in vitro. Recent studies also revealed partial TRPV1-agonist-like effects of I-RTX in the thermoregulatory system in mice, increasing intracellular Ca2+ concentrations. It also exerts weak, partial agonism on recombinant TRPV1 in vitro.

Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties. It behaves as a 5-HT1A receptor partial agonist (Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor receptor antagonist (Ki = 14 nM), and also has weak affinity for the sigma receptor (Ki = 558 nM). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation, cognitive/memory impairment, catalepsy, and extrapyramidal symptoms.

HU-243 (AM-4056) is a synthetic cannabinoid drug that is a single enantiomer of the hydrogenated derivative of the commonly used reference agonist HU-210. It is a methylene homologue of canbisol. It is a potent agonist at both the CB1 and CB2 receptors, with a binding affinity of 0.041 nM at the CB1 receptor, making it marginally more potent than HU-210, which had an affinity of 0.061 nM in the same assay.

When used in conjunction with oocyte or embryo cryopreservation, using GnRH agonist rather than hCG for final maturation induction has no evidence of a difference in live birth rate (in contrast to fresh cycles where usage of GnRH agonist has a lower live birth rate). Anticoagulant prophylaxis is recommended to be administered only to selected subgroups of women such as those with other risk factors of hypercoagulability or those who do develop early OHSS.

Taspoglutide is a pharmaceutical drug, a glucagon-like peptide-1 agonist (GLP-1 agonist), under investigation for treatment of type 2 diabetes being codeveloped by Ipsen and Roche. Two phase II trials reported it was effective and well tolerated. Of the eight planned phase III clinical trials of weekly taspoglutide (four against exenatide, sitagliptin, insulin glargine, and pioglitazone), at least five were active in 2009. Preliminary results in early 2010 were favourable.

Fenoterol is a β adrenoreceptor agonist. It is classed as sympathomimetic β2 agonist and an inhaled bronchodilator asthma medication. Fenoterol is produced and sold by Boehringer Ingelheim as Berotec N and in combination with ipratropium as Berodual N. It was patented in 1962 and came into medical use in 1971 but, in the 1980s, concerns emerged about its safety and its use being associated with an increased risk of death (see below).

The histaminergic neurons have a very important role in preserving consciousness and in helping maintain wakefulness and remain active during cataplexy. In narcolepsy, there seems to be an increase in these neurons, possibly to compensate for hypocretin loss. A promising therapy would be to increase the activation of histaminergic neurons by an inverse agonist of the histamine H3 receptor, which enhances histamine release in hypothalamus. An inverse agonist of the histamine H3 is Pitolisant.

AM-855 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is a derivative of Δ8Tetrahydrocannabinol with a conformationally restricted side chain which has been bound into a fourth ring fused to the aromatic A-ring of the cannabinoid skeleton. AM-855 is an agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 22.3 nM at CB1 and 58.6 nM at CB2.

The recommended pain medication is usually a non-steroidal anti-inflammatory drug (NSAID), such as naproxen. Taking the active component of the birth control pill continuously or using an intrauterine device with progestogen may also be useful. Gonadotropin- releasing hormone agonist (GnRH agonist) may improve the ability of those who are infertile to get pregnant. Surgical removal of endometriosis may be used to treat those whose symptoms are not manageable with other treatments.

It is still the agonist, because while resisting gravity during relaxing, the triceps brachii continues to be the prime mover, or controller, of the joint action. Agonists are also interchangeably referred to as "prime movers," since they are the muscles considered primarily responsible for generating or controlling a specific movement. Another example is the dumbbell curl at the elbow. The "elbow flexor" group is the agonist, shortening during the lifting phase (elbow flexion).

It has six different stereoisomers which have varying properties. Four are inactive, but the 1S-(R,R)-disecbutyl isomer is a μ-opioid full agonist around 5.5 times more potent than morphine and the 1S-(S,S)-disecbutyl isomer is an antagonist. Since vimonol is supplied as a racemic mixture of isomers, the overall effect is a mixed agonist–antagonist profile similar to that of opioids such as pentazocine, although with somewhat fewer side effects.

Each AMPAR has four sites to which an agonist (such as glutamate) can bind, one for each subunit. The binding site is believed to be formed by the N-terminal tail and the extracellular loop between transmembrane domains three and four. When an agonist binds, these two loops move towards each other, opening the pore. The channel opens when two sites are occupied, and increases its current as more binding sites are occupied.

Although estriol is an estrogen, it has also been reported to have mixed agonist–antagonist or partial agonist activity at the ERs. On its own, it is said to be weakly estrogenic, but in the presence of estradiol, it has been found to be antiestrogenic. However, this is again due to the fact that estriol is a "short-acting" estrogen. If estriol is present continuously with estradiol, it shows no antagonism of estradiol.

CY-208,243 is a drug which acts as a dopamine agonist selective for the D1 subtype. Unlike most D1-selective agonists, it shows efficacy in animal models of Parkinson's disease.

Another countermeasure includes administration of midodrine, which is a selective alpha-1 adrenergic agonist. Midodrine produces arterial and venous constriction resulting in an increase in blood pressure by baroreceptor reflexes.

Deslorelin, sold under the brand names Ovuplant, SucroMate, and Suprelorin among others, is an injectable gonadotropin releasing hormone superagonist (GnRH agonist) which is used in veterinary medicine for various indications.

Other nAChR antagonists may serve as effective antidotes for this particular type of poisoning, as they would block nAChR to prevent the acetylcholine agonist from binding to the acetylcholine receptors.

5-Ethyl-N,N-dimethyltryptamine is a tryptamine derivative which acts as an agonist at the 5-HT1A and 5-HT1D serotonin receptors, with around 3x selectivity for 5-HT1D.

First description of changes in distribution of agonist excited receptors in membranes in real time.Bennett, M.R. (1972). Autonomic Neuromuscular Transmission. Monograph of the Physiological Society No. 30, Cambridge University Press.

Murodermin (INN), also known as recombinant murine epidermal growth factor (rmEGF), is a recombinant form of mouse epidermal growth factor (EGF) and an EGF receptor agonist which was never marketed.

FDU-PB-22 is an derivative of JWH-018 that is presumed to be a potent agonist of the CB1 receptor and has been sold online as a designer drug.

TC-2216 is a drug developed by Targacept which acts as a partial agonist at neural nicotinic acetylcholine receptors and is being researched for the treatment of anxiety and depression.

Frovatriptan is a 5HT receptor agonist, with high affinity for the 5-HT1B/1D receptors. It has no significant effects on the GABAA mediated channel activity and benzodiazepine binding sites.

CP-135807 is a drug which acts as a potent and selective agonist for the 5-HT1D serotonin receptor, and is used to study the function of this receptor subtype.

CUMYL-CBMINACA (SGT-277) is an indazole-3-carboxamide based synthetic cannabinoid receptor agonist that has been sold as a designer drug, first being identified in Germany in February 2020.

Lergotrile is an ergoline derivative which acts as a dopamine receptor agonist. It was developed for the treatment of Parkinson's disease, but failed in clinical trials due to liver toxicity.

Discovered in 2000, NADA preferentially binds to the CB1 receptor. Like anandamide, NADA is also an agonist for the vanilloid receptor subtype 1 (TRPV1), a member of the vanilloid receptor family.

Valerenic acid, a constituent of valerian root, has been found to act as a 5-HT5A receptor agonist, and this action could be involved in the sleep-promoting effects of valerian.

Youn et al. Molecular cloning of leukotactin-1: a novel human beta-chemokine, a chemoattractant for neutrophils, monocytes, and lymphocytes, and a potent agonist at CC chemokine receptors 1 and 3.

Berefrine (INN, USAN), also known as burefrine, is a sympathomimetic and mydriatic agent that was never marketed. It is an oxazolidine prodrug of phenylephrine, and hence, an α1-adrenergic receptor agonist.

Eluxadoline is a μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist that acts locally in the enteric nervous system, possibly decreasing adverse effects on the central nervous system.

Figure 2. Chemical structure of capsaicin Capsaicin (fig. 2), a naturally occurring vanilloid, is the best known TRPV1 agonist. Resiniferatoxin (RTX) is another naturally occurring vanilloid that exhibits TRPV1 agonistic activity.

25B-NBF (2C-B-NBF, NBF-2C-B) is a derivative of the phenethylamine hallucinogen 2C-B, which acts as a highly potent partial agonist for the human 5-HT2A receptor.

25C-NBF (2C-C-NBF, NBF-2C-C) is a derivative of the phenethylamine hallucinogen 2C-C, which acts as a highly potent partial agonist for the human 5-HT2A receptor.

Binospirone (MDL-73,005-EF) is a drug which acts as a partial agonist at 5-HT1A somatodendritic autoreceptors but as an antagonist at postsynaptic 5-HT1A receptors. It has anxiolytic effects.

Premazepam is a benzodiazepine derivative. It is a partial agonist of benzodiazepine receptors and was shown in 1984 to possess both anxiolytic and sedative properties in humans but was never marketed.

Heidmann T., Changeux J.-P. (1979). Fast kinetic studies on the interaction of a fluorescent agonist with the membrane-bound acetylcholine receptor from T. marmorata. Eur. J. Biochem. 94: 255-279.

Selective galanin agonists are anticonvulsant, while antagonists produce antidepressant and anxiolytic effects in animals, so either agonist or antagonist ligands for the galanin receptors may be potentially therapeutic compounds in humans.

DHE's antimigraine activity is due to its action as an agonist to the serotonin (5-HT) -1B, -1D and -1F receptors. It also interacts with other serotonin, adrenergic and dopamine receptors.

A ligand that can bind to and alter the function of the receptor that triggers a physiological response is called a receptor agonist. Ligands that bind to a receptor but fail to activate the physiological response are receptor antagonists. Two agonists with similar binding affinity Agonist binding to a receptor can be characterized both in terms of how much physiological response can be triggered (that is, the efficacy) and in terms of the concentration of the agonist that is required to produce the physiological response (often measured as EC50, the concentration required to produced the half-maximal response). High-affinity ligand binding implies that a relatively low concentration of a ligand is adequate to maximally occupy a ligand-binding site and trigger a physiological response.

A Cochrane review of autologous oocyte transfers estimated that GnRH agonist, compared to hCG, gives an odds ratio of pregnancy of approximately 0.47. It estimated that, for a woman with a 31% chance of achieving live birth with the use of hCG, the chance of a live birth with the use of an GnRH agonist would be between 12% and 24%. Likewise, using GnRH agonist instead of hCG was associated with a lower ongoing pregnancy rate (pregnancy beyond 12 weeks) than was seen with HCG (odds ratio 0.70) and a higher rate of early (less than 12 weeks) miscarriage (odds ratio 1.74). However, a higher pregnancy rate when using hCG is only found in those receiving luteal support without luteinizing hormone activity (such as progesterone or progestin).

Originally synthesized by chemist Wayne E. Kenney, BAY 38-7271 (KN 38-7271) is a drug which is a cannabinoid receptor agonist developed by Bayer AG. It has analgesic and neuroprotective effects and is used in scientific research, with proposed uses in the treatment of traumatic brain injury. It is a full agonist with around the same potency as CP 55,940 in animal studies, and has fairly high affinity for both CB1 and CB2 receptors, with Ki values of 2.91nM at CB1 and 4.24nM at CB2. It has been licensed to KeyNeurotek Pharmaceuticals for clinical development,Pipeline and was in Phase II trials in 2008KeyNeurotek Pharmaceuticals AG Reports Positive Phase I Data of Its Cannabinoid Receptor- Agonist but its development appears to have stopped.

The mixed agonists-antagonists drug class exerts their analgesic actions by agonistic activity at the KOR. While all drugs in this class possess MOR antagonistic activity leading to less abuse potential, nalbuphine is the only approved drug in the mixed agonist-antagonist class listed in terms of its pharmacological actions and selectivities on opioid receptors as a MOR partial agonist or antagonist as well as a KOR agonist (Gustein et al. 2001). Nubain was approved for marketing in the United States in 1978 and remains as the only opioid analgesic of this type (marketed in the U.S.) not controlled under the Controlled Substances Act (CSA). When the Controlled Substances Act (CSA) was enacted in 1971, nalbuphine was placed in schedule II. Endo Laboratories, Inc.

A common mechanism for agonists is reuptake inhibition, where the agonist blocks neurotransmitters from reentering the pre-synaptic axon terminal. This gives the neurotransmitter more time in the synaptic cleft to act on the synaptic receptors. Conversely, antagonists often bind directly to receptors in the synaptic cleft, effectively blocking neurotransmitters from binding. At the alpha adrenoceptors, (R)-3-nitrobiphenyline is an α2C selective agonist as well as being a weak antagonist at the α and α subtypes.

Formoterol, also known as eformoterol, is a long-acting β2 agonist (LABA) used as a bronchodilator in the management of asthma and chronic obstructive pulmonary disease (COPD). Formoterol has an extended duration of action (up to 12 h) compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4 h to 6 h. LABAs such as formoterol are used as "symptom controllers" to supplement prophylactic corticosteroid therapy. A "reliever" short-acting β2 agonist (e.g.

Endocannabinoid 2-arachidonoylglycerol (2-AG), which is 170-fold more abundant in the brain than AEA, acts as a full agonist at both CB receptors. CBD is a phytocannabinoid that acts as a rather weak antagonist at both CBRs and a more potent agonist at TRPV1 and antagonist at TRPM8. It is also known to be a negative allosteric modulator at CB1. CBD has been found to counteract some of the negative side effects of THC.

Dihydrexidine (DAR-0100) is a moderately selective full agonist at the dopamine D1 and D5 receptors. It has approximately 10-fold selectivity for D1 and D5 over the D2 receptor. Although dihydrexidine has some affinity for the D2 receptor, it has functionally selective (highly biased) D2 signaling, thereby explaining why it lacks D2 agonist behavioral qualities. Dihydrexidine has shown impressive antiparkinson effects in the MPTP-primate model, and has been investigated for the treatment of Parkinson's disease.

The IC50 of a drug can be determined by constructing a dose-response curve and examining the effect of different concentrations of antagonist on reversing agonist activity. IC50 values can be calculated for a given antagonist by determining the concentration needed to inhibit half of the maximum biological response of the agonist. IC50 values can be used to compare the potency of two antagonists. IC50 values are very dependent on conditions under which they are measured.

2C-H exhibits agonist activity in vitro at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization. 2C-H was found to be inactive in NCI In Vivo Anticancer Drug Screens for tumor model L1210 Leukemia. It was found to be an active Alpha-1 adrenergic receptor agonist in rabbit ear arteries. It has binding affinity towards 5-HT2C and 5-HT2A receptors in rats.

Tryptamine is an agonist of hTAAR1. It acts as a non-selective serotonin receptor agonist and serotonin-norepinephrine-dopamine releasing agent (SNDRA), with a preference for evoking serotonin and dopamine release over norepinephrine release. Tryptamine has been shown to act as a noncompetitive inhibitor of serotonin N-acetyltransferase (SNAT) in mosquitoes. SNAT catalyzes the anabolic metabolism of serotonin into N-acetylserotonin, another neuromodulator (specifically a neurotrophic factor via TrkB agonism) and the immediate precursor for melatonin.

Isoprenaline is a β1 and β2 adrenoreceptor agonist and has almost no activity on alpha adrenergic receptors. Its agonist effects at TAAR1 provide it with a pharmacodynamic effects that resemble those of the endogenous trace amines, like tyramine. "Table 1: EC50 values of different agonists at hTAAR1, hADRB1 and hADRB2." Isoprenaline's effects on the cardiovascular system (non-selective) relate to its actions on cardiac β1 receptors and β2 receptors on smooth muscle within the tunica media of arterioles.

GR-89696 is a drug which acts as a highly selective κ-opioid agonist. It shows selective effects in different animal models and it is thought it may be a subtype-selective agonist for the κ2 subtype. Recent studies have suggested that GR-89696 and related κ2-selective agonists may be useful for preventing the itching which is a common side effect of conventional opioid analgesic drugs, without the additional side effects of non-selective kappa agonists.

5-Fluoro-N,N-dimethyltryptamine (5-fluoro-DMT) is a tryptamine derivative related to compounds such as 5-bromo-DMT and 5-MeO-DMT. Fluorination of psychedelic tryptamines either reduces or has little effect on 5-HT2A/C receptor affinity or intrinsic activity, although 6-fluoro-DET is inactive as a psychedelic despite acting as a 5-HT2A agonist (cf. lisuride), while 4-fluoro-5-methoxy-DMT is a much stronger agonist at 5-HT1A than 5-HT2A.

5-Fluorowillardiine is a selective agonist for the AMPA receptor, with only limited effects at the kainate receptor. It is an excitotoxic neurotoxin when used in vivo and so is rarely used in intact animals, but it is widely used to selectively stimulate AMPA receptors in vitro. It is structurally similar to the compound willardiine, which is also an agonist for the AMPA and kainate receptors. Willardiine occurs naturally in Mariosousa willardiana and Acacia sensu lato.

DOM is a selective 5-HT2A, 5-HT2B, and 5-HT2C receptor partial agonist. Its psychedelic effects are mediated by its agonistic properties at the 5-HT2A receptor. Due to its selectivity, DOM is often used in scientific research when studying the 5-HT2 receptor subfamily. DOM is a chiral molecule, and R-(−)-DOM is the more active enantiomer, functioning as a potent agonist of the serotonin 5-HT family of receptors; mainly of the 5-HT2 subtype.

Figure 4: The chemical structures of MK-801, phencyclidine and ketamine, high affinity uncompetitive NMDA receptor antagonists. Uncompetitive NMDA receptor antagonists block within the ion channel at the Mg2+ site (pore region) and prevent excessive influx of Ca2+. Noncompetitive antagonism refers to a type of block that an increased concentration of glutamate cannot overcome, and is dependent upon prior activation of the receptor by the agonist, i.e. it only enters the channel when it is opened by agonist.

NMP-7 is a drug which acts as both a non-selective agonist of the CB1 and CB2 cannabinoid receptors, and also as a blocker of T-type calcium channels, the target of anticonvulsant drugs such as ethosuximide. NMP-7 has an agonist EC50 of 96.9nM at CB1 and 10.5nM at CB2, and an IC50 of 1.84μM for blocking Cav3.2 T-type calcium channels. In animal studies it produces potent analgesic effects in a variety of different tests.

Progesterone is a progestogen, or an agonist of the nuclear progesterone receptors (PRs), the PR-A, PR-B, and PR-C. In addition, progesterone is an agonist of the membrane progesterone receptors (mPRs), including the mPRα, mPRβ, mPRγ, mPRδ, and mPRϵ. Aside from the PRs and mPRs, progesterone is a potent antimineralocorticoid, or antagonist of the mineralocorticoid receptor, the biological target of the mineralocorticoid aldosterone. In addition to its activity as a steroid hormone, progesterone is a neurosteroid.

It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing an α3 subunit. In rats 5′-hydroxypagoclone was identified as a major metabolite. This metabolite has a considerably greater efficacy at the α1 subtype than the parent compound and was shown to have significant anxiolytic-like activity and to produce sedation. In contrast to zopiclone, pagoclone produces anxiolytic effects with little sedative or amnestic actions at low doses.

EP44 receptors are expressed in the cochlea of the inner ear. Pre- and post-treatment of guinea pigs with an EP4 agonist significantly attenuated threshold shifts of auditory brain stem responses and significantly reduced the loss of outer hair cells caused by prior noise exposure. These findings indicate that EP4 is involved in mechanisms for prostaglandin E(1) actions on the cochlea, and local EP4 agonist treatment may be a means for attenuating noise-induced hearing lose.

Like montelukast, zafirlukast antagonizes bronchoconstrictive by selectively antagonising the CysLT1 receptor and affects all of the leukotrienes (LTC4, LTD4, and LTE4). The qualitative structural requirements and pharmacophore for CysLT1 antagonists were designed from the structural similarity of the agonist LTD4. But that has its limitations as agonist and antagonist do not necessarily bind in the same manner nor to the same site. So the importance of certain moiety may be overestimated and some moieties may be overlooked.

EE is a synthetic estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. It also has functional antiandrogenic effects by decreasing the circulating free fractions of androgens. CPA is a progestin (synthetic progestogen), or an agonist of the progesterone receptors, the biological target of progestogens like progesterone. It also acts as an antiandrogen, or as an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone.

Ractopamine is an animal feed additive used to promote leanness and increase food conversion efficiency in livestock in some countries, but banned in others. Pharmacologically, it is a phenol-based TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors. It is most commonly administered to animals for meat production as ractopamine hydrochloride. It is the active ingredient in products marketed in the US as Paylean for swine, Optaflexx for cattle, and Topmax for turkeys.

Chemical structure of terbutaline Terbutaline is a type of sympathomimetic drug. Terbutaline is a selective β2 receptor agonist that is clinically used to treat asthma. Since terbutaline is an agonist selective to β2 receptors, it activates β2 receptors in smooth muscles and stimulates sympathetic responses, including the increased relaxation of smooth muscles. Relaxation of smooth muscles in bronchi and trachea provides the effect of airway widening and hence can be served as a bronchodilator for asthma treatment.

Ciladopa (AY-27,110) is a dopamine agonist with a similar chemical structure to dopamine. It was under investigation as an antiparkinsonian agent but was discontinued due to concerns of tumorogenesis in rodents.

It behaves as a partial agonist at the 5-HT2A receptor. MEM is relatively selective for these sites and displays low/negligible (> 10,000 nM) affinity for a wide array of other targets.

Another alternative to this is that the 5-HT4 agonist currently available for use in humans do not have great enough potency or bioavailability in the brain to elicit the same effects.

CUMYL-CH-MEGACLONE (CUMYL-CHMGACLONE, SGT-270) is a gamma-carboline based synthetic cannabinoid receptor agonist that has been sold as a designer drug, first being identified in Hungary in December 2018.

Amthamine is a histamine agonist selective for the H2 subtype. It has been used in vitro and in vivo to study gastric secretion, as well as other functions of the H2 receptor.

Models of the extracellular domain of the nicotinic receptors and of agonist and Ca++ binding sites. Proc. Natl. Acad. Sci. USA, 99: 3210-3215.Galzi J.-L., Bertrand S., Corringer P.-J.

Galmic is a drug which acts as a selective, non-peptide agonist at the galanin receptors GALR. It has anticonvulsant, antidepressant and analgesic effects in animal studies, but also inhibits memory functions.

Triamcinolone acetonide is a corticosteroid. It is specifically a glucocorticoid, or an agonist of the glucocorticoid receptor, that is about five times as potent as cortisol. It has very little mineralocorticoid effects.

MLGA is a progestogen, and hence is an agonist of the progesterone receptor. It has been found to possess 73% of the affinity of progesterone for the progesterone receptor in rhesus monkey uterus.

Divaplon (RU-32698) is a nonbenzodiazepine, anxiolytic and anticonvulsant drug from the pyrazolopyrimidine family of drugs. It acts as a partial agonist at the "benzodiazepine site" of the GABAA receptor in the brain.

TC OT 39 is a non-peptide partial agonist of the oxytocin and vasopressin V2 receptors (Ki = 147 nM and >1000 nM, respectively) and antagonist of the vasopressin V1A receptor (Ki = 330 nM).

The idea behind counterstrain states that tender points result from reflexive muscular spasm that correspond to dysfunctional motor segments, due to the compensation of an antagonist muscle responding to agonist muscle over-lengthening.

Lixisenatide (trade name Lyxumia in the European Union and Adlyxin in the U.S. and manufactured by Sanofi) is a once-daily injectable GLP-1 receptor agonist for the treatment of type 2 diabetes.

Metoclopramide appears to bind to dopamine D2 receptors with nanomolar affinity (Ki = 28.8 nM), where it is a receptor antagonist, and is also a mixed 5-HT3 receptor antagonist/5-HT4 receptor agonist.

2-Chloro-5-hydroxyphenylglycine or CHPG is an agonist of the metabotropic glutamate receptors, specific for mGluR5. It is capable of directly potentiating the depolarization of hippocampal CA1 neurons induced through NMDA administration.

Aminoalkylindoles (AAIs) are a family of cannabinergic compound that act as a cannabinoid receptor agonist. They were invented by pharmaceutical company Sterling-Winthrop in the early 1990s as potential nonsteroidal anti- inflammatory agents.

All Kir channels require phosphatidylinositol 4,5-bisphosphate (PIP2) for activation. PIP2 binds to and directly activates Kir 2.2 with agonist-like properties. In this regard Kir channels are PIP2 ligand-gated ion channels.

Cevimeline (trade name Evoxac) is a parasympathomimetic and muscarinic agonist, with particular effect on M1 and M3 receptors. It is used in the treatment of dry mouth and especially associated with Sjögren's syndrome.

BP-897 is a drug used in scientific research which acts as a moderately selective dopamine D3 receptor partial agonist. It has mainly been used in the study of treatments for cocaine addiction.

For this reason, AOX genes are becoming increasingly important to both understand and control in the therapeutic drug industry. Pfizer TLR7 agonist program has found several techniques to switch the AO metabolism off.

RS-56812 is a potent and selective partial agonist at the 5HT3 receptor. It has been shown to improve performance on animal tests of memory. Its use in humans is not well documented.

2-Methyl-5-hydroxytryptamine (2-Methylserotonin, 2-Methyl-5-HT) is a tryptamine derivative closely related to the neurotransmitter serotonin which acts as a moderately selective full agonist at the 5-HT3 receptor.

SB-204070 is a drug which acts as a potent and selective 5-HT4 serotonin receptor antagonist (or weak partial agonist), and is used for research into the function of this receptor subtype.

NM-2201 acts as a full agonist with a binding affinity of 0.332 nM at CB1 and 0.732 nM at CB2 cannabinoid receptors. It has been linked to serious adverse events in users.

Expression of L-CaBP1 also help in the inhibition of histamine-induced [Ca2+] oscillations in HeLa cells. L-CaBP1 is able to specifically regulate InsP3 receptor-mediated alterations in [Ca2+] during agonist stimulation.

DPI-221 is an opioid drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces fewer convulsions than most drugs from this family.

XCT-790 is a potent and selective inverse agonist ligand of the estrogen- related receptor alpha (ERRα). Independent of its inhibition of ERRα, XCT-790 is a potent mitochondrial electron transport chain uncoupler.

Magnesium sulfate may be used as bronchodilator after beta-agonist and anticholinergic agents have been tried, e.g. in severe exacerbations of asthma,. The salt can be administered by nebulization or by intravenous injection.

Ergocornine is a crystalline ergopeptine and one of the ergot alkaloids separated from ergotoxine. It is also a dopamine receptor agonist. It was discovered by Albert Hofmann, the Swiss chemist who created LSD.

For synaptic receptors, an agonist is a compound that increases the activation of the receptor by binding directly to it or by increasing the amount of time neurotransmitters are in the synaptic cleft. An antagonist is a compound that has the opposite effect of an agonist. It decreases the activation of a synaptic receptor by binding and blocking neurotransmitters from binding or by decreasing the amount of time neurotransmitters are in the synaptic cleft. These actions can be achieved via multiple mechanisms.

Abediterol (INN; development codes AZD-0548 and LAS 100977) is a once-daily experimental drug candidate for the treatment of asthma and chronic obstructive pulmonary disease (COPD). It is currently under development by the Spanish pharmaceutical company Almirall and is in Phase II clinical trials.Product development pipeline, Almirall It acts as a dual β2 adrenergic agonist and muscarinic antagonist and is classified as an ultra-long-acting β2 agonist (ultra-LABA). Its coformulation with mometasone furoate is also in Phase II clinical trials.

L-759,656 is an analgesic drug that is a cannabinoid agonist. It is a highly selective agonist for the CB2 receptor, with selectivity of 414x for CB2 over CB1, although it is still not as selective as newer agents such as HU-308. It produces some similar effects to other cannabinoid agonists such as analgesia, but with little or no sedative or psychoactive effects due to its weak CB1 activity, and a relatively strong antiinflammatory effect due to its strong activity at CB2.

Dihydroergocryptine (DHEC, trade names Almirid, Cripar) is a dopamine agonist of the ergoline chemical class that is used as an antiparkinson agent. Dihydroergocryptine has been shown to be particularly effective as monotherapy in the early stages of Parkinson's disease. Initial monotherapy with a dopamine agonist (other examples include pergolide, pramipexole, and ropinirole) is associated with reduced risk for motor complications in Parkinson patients relative to levodopa. DHEC, like other dopamine agonists, aims to mimic the endogenous neurotransmitter and exert an antiparkinsonian effect.

Several in vitro and in vivo studies have demonstrated that dihydroergocriptine is an effective anti-Parkinson drug, most likely exerting its effects as a potent agonist of D2 receptors. The Kd of DHEC is found to be around 5-8 nM at D2 receptors. Less certain is the contribution of its partial D1 receptor and D3 receptor agonist activity. DHEC has a lower affinity for D1 and D3 receptors (Kd is around 30 nM for both) than for D2 receptors.

Lorcaserin is the only agent that has completed phase III clinical trials, and achieved US Food and Drug Administration (FDA) approval. However it was later withdrawn from the market in February 2020 due to a higher risk of malignancy in a randomized trial of lorcaserin. Previously approved agents were subsequently removed from the US market. Lorcaserin is a full agonist for 5-HT2C and 5-HT2B receptors and partial agonist for 5-HT2A receptors (75% of the maximal response elicited by serotonin).

Opioid effects (adverse or otherwise) can be reversed with an opioid antagonist such as naloxone or naltrexone. These competitive antagonists bind to the opioid receptors with higher affinity than agonists but do not activate the receptors. This displaces the agonist, attenuating or reversing the agonist effects. However, the elimination half-life of naloxone can be shorter than that of the opioid itself, so repeat dosing or continuous infusion may be required, or a longer acting antagonist such as nalmefene may be used.

Sumatriptan is structurally similar to serotonin (5-HT), and is a 5-HT receptor (types 5-HT1D and 5-HT1B ) agonist. Sumatriptan's primary therapeutic effect, however, is in its inhibition of the release of Calcitonin gene-related peptide (CGRP), likely through its 5-HT1D/1B receptor-agonist action. This is substantiated by the efficacy of newly developed CGRP antagonists and antibodies in the preventative treatment of migraine. However, how agonism of the 5-HT1D/1B receptors inhibits CGRP release is not fully understood.

Gabapentin, an indirect GABA modulator, has shown some preliminary benefit for reducing cravings and cannabis use. The agonist substitution approach is one that draws upon the analogy of the success of nicotine replacement therapy for nicotine addiction. Dronabinol, which is synthetic THC, has shown benefit in reducing cravings and other symptoms of withdrawal, though without preventing relapse or promoting abstinence. Combination therapy with dronabinol and the alpha 2 adrenergic receptor agonist lofexidine have shown mixed results, with possible benefits towards reducing withdrawal symptoms.

The muscle performing an action is the agonist, while the muscle which contraction brings about an opposite action is the antagonist. For example, an extension of the lower arm is performed by the triceps as the agonist and the biceps as the antagonist (which contraction will perform flexion over the same joint). Muscles that work together to perform the same action are called synergists. In the above example synergists to the biceps can be the brachioradialis and the brachialis muscle.

4-NEMD is a potent sedative drug which acts as a selective alpha-2 adrenergic agonist. It is closely related to dexmedetomidine but is several times more potent. Like other alpha-2 agonists, it produces sedative and muscle relaxant effects but without producing respiratory depression. It is not currently used in medicine but has been researched as the basis for a potential new generation of alpha-2 agonist drugs, which may have selectivity for the different subtypes of the alpha-2 receptor.

Competitive NMDA receptor antagonists, which were developed first, are not a good option because they compete and bind to the same site (NR2 subunit) on the receptor as the agonist, glutamate, and therefore block normal function also. They will block healthy areas of the brain prior to having an impact on pathological areas, because healthy areas contain lower levels of agonist than pathological areas. These antagonists can be displaced from the receptor by high concentration of glutamate which can exist under excitotoxic circumstances.

In preliminary studies, 3 Korean patients with periorbital vitiligo (i.e. skin blanching) were treated topically with the FP receptor agonist, latanoprost, for two months; the three patients experienced 20%, 50%, and >90% re- pigmentation of their vitiligo lesions. Fourteen patients with hypopigmented in their scarreed tissues were treated with the FP receptor agonist, bimatoprost, applied topically plus laser therapy and topical tretinoin or pimecrolimus. Most patients demonstrated significant improvement in their hypopigmentation, but the isolated effect of topical bimatoprost was not evaluated.

Bromo-DragonFLY also has a high binding affinity for the 5-HT2B and 5-HT2C serotonin receptors, and is most accurately described as a non-subtype selective 5-HT2 agonist, as it is actually twice as potent an agonist for 5-HT2C receptors as for 5-HT2A, as well as being less than 5x selective for 5-HT2A over 5-HT2B. Bromo-DragonFLY is also a MAO-A inhibitor, and thus strongly inhibits oxidative deamination of 5-HT, increasing its risk profile.

Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the GABA antagonist flumazenil, although its effects are somewhat different. It is classified as a high- potency benzodiazepine due to its high affinity binding to benzodiazepine binding sites where it acts as a partial agonist. Its profile as a partial agonist and preclinical trial data suggests that it may have a reduced adverse effect profile.

Enadoline is a drug which acts as a highly selective κ-opioid agonist. In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of salvinorin A. It was studied as a potential analgesic, but abandoned because of the dose-limiting effects of dysphoria, which could be expected from a κ-opioid agonist. There was mention of its potential in treating comatose head injury or stroke victims, where that type of side effect would be immaterial.

AM-906 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is conformationally restricted by virtue of the double bond on its side chain, leading an increased affinity for and selectivity between CB1 and CB2 receptors. It is a potent and selective agonist for the CB1 cannabinoid receptor, with a Ki of 0.8 nM at CB1 and 9.5 nM at CB2, a selectivity of almost 12x. The corresponding E or trans isomer is AM-905.

L-163,491 is a drug which acts as a partial agonist of angiotensin II receptor type 1, and with lower affinity as an agonist of angiotensin II receptor type 2, mimicking the action of angiotensin II. Its practical applications to date have been limited to scientific research into the function of the angiotensin receptor system, but it has been suggested as a potential therapeutic agent for the treatment of inflammation of the lungs associated with certain viral diseases such as COVID-19.

NAS has been shown to act as a potent TrkB receptor agonist, while serotonin and melatonin do not. Subchronic and chronic administration of NAS to adult mice induces proliferation of neural progenitor cells (NPC)s, blockage of TrkB abolished this effect suggesting that it is TrkB-dependent. NAS was also found to significantly enhance NPC proliferation in sleep- deprived mice. It is thought that the anti-depressant and neurotrophic effects of NAS are in part due to its role as a TrkB agonist.

A number of drugs that work through nuclear receptors display an agonist response in some tissues and an antagonistic response in other tissues. This behavior may have substantial benefits since it may allow retaining the desired beneficial therapeutic effects of a drug while minimizing undesirable side effects. Drugs with this mixed agonist/antagonist profile of action are referred to as selective receptor modulators (SRMs). Examples include Selective Androgen Receptor Modulators (SARMs), Selective Estrogen Receptor Modulators (SERMs) and Selective Progesterone Receptor Modulators (SPRMs).

Kainic acid, or kainate, is an acid that naturally occurs in some seaweed. Kainic acid is a potent neuroexcitatory amino acid agonist that acts by activating receptors for glutamate, the principal excitatory neurotransmitter in the central nervous system. Glutamate is produced by the cell's metabolic processes and there are four major classifications of glutamate receptors: NMDA receptors, AMPA receptors, kainate receptors, and the metabotropic glutamate receptors. Kainic acid is an agonist for kainate receptors, a type of ionotropic glutamate receptor.

Nafarelin is a GnRH agonist, or an agonist of the GnRH receptor, the biological target of GnRH. It works by continuously activating the GnRH receptor, which results in profound desensitization of the receptor such that it becomes non-functional. As a result, nafarelin suppresses the GnRH-induced secretion of the gonadotropins, luteinizing hormone and follicle-stimulating hormone, from the pituitary gland. This, in turn, results in profound suppression of gonadal sex hormone production, as well as reversible suppression of fertility.

Orexin-A ( hypocretin-1) has been shown to be strongly wake-promoting in animal models, but unfortunately it does not cross the blood-brain barrier. Therefore, companies have developed orexin receptor antagonists, like suvorexant, for the treatment of insomnia. It is also likely that an orexin-A receptor agonist will be found and developed for the treatment of hypersomnia. In August 2015, Nagahara et al published their work in synthesizing the first HCRT/OX2R agonist, compound 26, with good potency and selectivity.

When used as a food additive, ractopamine added to feed can be distributed by the blood to the muscle tissues, where it serves as a full agonist to murine TAAR1 (not necessarily human). It is also an agonist to beta-adrenergic receptors. A cascade of events will then be initiated to increase protein synthesis, which results in increased muscle fiber size. Ractopamine is known to increase the rate of weight gain, improve feed efficiency, and increase carcass leanness in finishing swine.

Nalmexone (INN) (code names EN-1620A, UM-592), or nalmexone hydrochloride (USAN), is a semisynthetic, opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties that was never marketed. In clinical studies it was found to have comparable analgesic efficacy to morphine, though with several-fold reduced potency. In addition, nalmexone's side effects, the most common of which were sleepiness and sweating, were reported to be similar to those of morphine, albeit with a noticeably higher degree of incidence.

25I-NBOH acts as a potent agonist for the 5HT2A receptor, with a Ki of 0.061 nM at the human 5HT2A receptor, similar to the better-known compound 25I-NBOMe, making it some twelve times the potency of 2C-I itself. Although in vitro tests show this compound acts as an agonist, animal studies to confirm these findings have not been reported. While the N-benzyl derivatives of 2C-I had significantly increased binding to 5HT2A receptor fragments, compared to 2C-I, the N-benzyl derivatives of DOI were less active compared to DOI. 25I-NBOH is notable as one of the most selective agonist ligands for the 5-HT2A receptor with an EC50 value of 0.074 nM with more than 400 times selectivity over the 5-HT2C receptor.

Functional selectivity has been proposed to broaden conventional definitions of pharmacology. Traditional pharmacology posits that a ligand can be either classified as an agonist (full or partial), antagonist or more recently an inverse agonist through a specific receptor subtype, and that this characteristic will be consistent with all effector (second messenger) systems coupled to that receptor. While this dogma has been the backbone of ligand- receptor interactions for decades now, more recent data indicates that this classic definition of ligand-protein associations does not hold true for a number of compounds; such compounds may be termed as mixed agonist- antagonists. Functional selectivity posits that a ligand may inherently produce a mix of the classic characteristics through a single receptor isoform depending on the effector pathway coupled to that receptor.

LCOR is a transcriptional corepressor widely expressed in fetal and adult tissues that is recruited to agonist-bound nuclear receptors through a single LxxLL motif, also referred to as a nuclear receptor (NR) box.

Ebalzotan (NAE-086) is a selective 5-HT1A receptor agonist. It was under development as an antidepressant and anxiolytic agent but produced undesirable side effects in phase I clinical trials and was subsequently discontinued.

Piribedil (trade names Pronoran, Trivastal Retard, Trastal, Trivastan, Clarium and others) is an antiparkinsonian agent and piperazine derivative which acts as a D2 and D3 receptor agonist. It also has α2-adrenergic antagonist properties.

AMB-CHMINACA or MMB-CHMINACA (also known as MA-CHMINACA) is an indazole-based synthetic cannabinoid that is a potent agonist of the CB1 receptor and has been sold online as a designer drug.

ABT-202 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors and has been researched for use as an analgesic, although it has not passed clinical trials.

Taxifolin showed promising pharmacological activities in the management of inflammation, tumors, microbial infections, oxidative stress, cardiovascular, and liver disorders Taxifolin has been found to act as an agonist of the adiponectin receptor 2 (AdipoR2).

Protokylol (Ventaire) is a β-adrenergic receptor agonist used as a bronchodilator in Europe and the United States. It is methylenedioxyphenyl- isoproterenol. The Para-Methoxyamphetamine (PMA) analog is twice the potency as the tenamfetamine analog.

The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. Macimorelin is a growth hormone secretagogue receptor (ghrelin receptor) agonist causing release of growth hormone from the pituitary gland.

5F-ADBICA (also known as 5F-ADB-PICA) is an indole-based synthetic cannabinoid that is a potent agonist at CB1 receptors and CB2 receptors with EC50 values of 0.77 nM and 1.2 nM respectively.

Phenylbiguanide (PBG) is a 5-HT3 agonist used to study the role of 5-HT3 receptors in the central nervous system. It has been found to trigger dopamine release in the nucleus accumbens of rats.

PD-168,077 is a drug which acts as a dopamine agonist selective for the D4 subtype, which is used for researching the role of D4 receptors in the brain, particularly relating to learning and memory.

PRE-084 is a sigma receptor agonist, selective for the σ1 subtype. It has nootropic and antidepressant actions in animal studies, as well as antitussive and reinforcing effects. PRE-084 increases the expression of GDNF.

A-41988 (BW29Y) is an analgesic drug which acts as a cannabinoid agonist. It was developed by Abbott Laboratories in the 1970s, and researched for potential use in the treatment of glaucoma, but never commercialised.

Medications used include levodopa or a dopamine agonist such as pramipexole. RLS affects an estimated 2.5–15% of the American population. Females are more commonly affected than males, and it becomes increasingly common with age.

Quipazine is a piperazine drug used in scientific research. It is a moderately selective serotonin receptor receptor agonist, binding to a range of different serotonin receptors, but particularly to the 5-HT2A and 5-HT3.

Zhang et al. 2005, p. abstract. However, it is an even more potent D2 receptor partial agonist, and it is likely this action plays a significant role in its effects as well.Seeman et al. 2009.

Alvameline (Lu 25-109) is a M1 receptor agonist and M2/M3 receptor antagonist that was under investigation for the treatment of Alzheimer's disease, but produced poor results in clinical trials and was subsequently discontinued.

WAY-629 is a 5-HT2C agonist that reduces feeding behavior when administered to rats. It was used as a starting point for developing more potent and selective 5-HT2C agonists aimed at treating obesity.

Thus, mu-opioid receptors induce relaxation, trust, satisfaction and have a strong analgesic effect. This system is also thought to be important in mediating complex social behaviors involved in the formation of stable, emotionally committed relationships. Social attachment was demonstrated to be mediated by the opioid system through experiments administering morphine and naltrexone, an opioid agonist and antagonist, to juvenile guinea pigs. The agonist decreased the preference of the juvenile to be near the mother and reduced distress vocalization whereas the antagonist had the opposite effects.

Channel blockers are antagonists for the channels required to produce normal physiological function in cells. Many channels have binding spots for regulatory elements which can promote or repress normal function depending on the requirements within the cell and organism. The normal function of agonist binding is the generation of cellular changes leading to various downstream effects; these effects range from altering membrane potential to initiation of signaling cascades. Conversely, when open channel blockers bind to the cell they prevent the normal function of agonist binding.

It has been reported that the effects of salvinorin A in mice are blocked by κ-opioid receptor antagonists. In addition, salvinorin A has recently been found to act as a D2 receptor partial agonist, with an affinity of 5–10 nM, an intrinsic activity of 40–60%, and an EC50 of 48 nM. This suggests that the D2 receptor may also play an important role in its effects. Salvinorin A shows atypical properties as an agonist of the KOR relative to other KOR agonists.

Liquiritigenin is a flavanone that was isolated from Glycyrrhiza uralensis, and is found in a variety of plants, including Glycyrrhiza glabra (licorice). It is an estrogenic compound which acts as a selective agonist of the ERβ subtype of the estrogen receptor (ER), though it is also reported to act as an ERα partial agonist at sufficient concentrations. It also has a choleretic effect. Liquiritigenin,NADPH:oxygen oxidoreductase (hydroxylating, aryl migration) is an enzyme that uses liquiritigenin, O2, NADPH and H+ to produce 2,7,4'-trihydroxyisoflavanone, H2O, and NADP+.

These are versatile agents with a wide range of possible pharmacological activities depending on the extent and range to which chemical modifications are implemented. The various choice of substitutions that are made allows for "fine-tuning" of the pharmacological profile that results. As examples, BTCP is a selective dopamine reuptake inhibitor, PCP is primarily an NMDA antagonist, and BDPC is a potent μ-opioid agonist, while PRE-084 is a selective sigma receptor agonist. Thus, radically different pharmacology is possible through different structural combinations.

In 1986, the first gene coding for a catecholamine receptor, the β2-adrenoceptor from hamster lung, was cloned by a group of sixteen scientists, among them Robert Lefkowitz and Brian Kobilka of Duke University in Durham, North Carolina. Genes for all mammalian catecholamine receptors have now been cloned, for the nine adrenoceptors α1A, α1B, α1D, α2A, α2B, α2C, β1, β2 and β3 and the five dopamine receptors D1, D2, D3, D4 und D5. Their fine structure, without agonist or agonist-activated, is being studied at high resolution.

The agonist that binds to the receptor and initiates the response is usually abbreviated A or D. At low agonist concentrations, [A], the response, E is immeasurably low but at higher [A], E becomes measurable. E increases with [A] until at sufficiently high [A], when E plateaus towards an asymptotic maximum attainable response, Emax. The [A] at which E is 50% of Emax is termed the half maximal effective concentration and is abbreviated EC50, or rarely [A]50. The term "potency" refers to the EC50 value.

When SPRMs bind to the progesterone receptor, the equilibrium between the two conformational states is more closely balanced and hence more easily perturbed by differences in the cellular environment. In tissues where the concentration of coactivators is higher than corepressors, the excess coactivators drive the equilibrium in the agonist direction. Conversely in tissues where corepressor concentration is higher the equilibrium is driven in the antagonist direction. Hence SPRMs display agonist activity in tissues where coactivators predominate and antagonist activity where corepressors are in excess.

BZP also acts as a non-selective serotonin receptor agonist on a wide variety of serotonin receptors; binding to 5HT2A receptors may explain its mild hallucinogenic effects at high doses, while partial agonist or antagonist effects at the 5HT2B receptors may explain some of BZPs peripheral side effects, as this receptor is expressed very densely in the gut, and binding to 5HT3 receptors may explain the common side effect of headaches, as this receptor is known to be involved in the development of migraine headaches.

Varenicline displays full agonism on α7 nicotinic acetylcholine receptors and is a partial agonist on the α4β2, α3β4, and α6β2 subtypes. In addition, it is a weak agonist on the α3β2 containing receptors. Varenicline's partial agonism on the α4β2 receptors rather than nicotine's full agonism produces less effect of dopamine release than nicotine's. This α4β2 competitive binding reduces the ability of nicotine to bind and stimulate the mesolimbic dopamine system—similar to the method of action of buprenorphine in the treatment of opioid addiction.

Vabicaserin has a high affinity for 5-HT2C receptors and low affinity for 5-HT2B and 5-HT2A receptors. Vabicaserin is a full agonist with approximately 4-fold greater selectivity for 5-HT2C over these related receptors, in terms of binding affinity. Vabicacserin is a full agonist in stimulating the 5-HT2C receptor; it was discovered when a class of tetrahydroquinoline-fused diazepines were being researched as possible potent 5-HT2C receptor agonists. As of 2012, vabicaserin is in clinical trials for the treatment of schizophrenia.

Dexanabinol (HU-211 or ETS2101) is a synthetic cannabinoid derivative in development by e-Therapeutics plc. It is the "unnatural" enantiomer of the potent cannabinoid agonist HU-210. Unlike other cannabinoid derivatives, HU-211 does not act as a cannabinoid receptor agonist, but instead has NMDA antagonist effects. It therefore does not produce cannabis-like effects, but is anticonvulsant and neuroprotective, and is widely used in scientific research as well as currently being studied for applications such as treating head injury, stroke, or cancer.

Indacaterol/glycopyrronium bromide/mometasone is indicated as a maintenance treatment of asthma in adults not adequately controlled with a maintenance combination of a long acting beta2 agonist and a high dose of an inhaled corticosteroid who experienced one or more asthma exacerbations in the previous year. Indacaterol is a long-acting beta-2 adrenergic receptor agonist. It relaxes the muscle around the airways into the lungs by activating targets called beta-2 receptors in the muscle cells. This helps to keep the airways open.

SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/D5 receptor full agonist. SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine. SKF-82,958 was also subsequently found to act as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen.

LH has a much shorter half- life than hCG, so that nearly all of the LH is cleared by the time of egg collection, or about 36 hours after trigger. Any developing signs of OHSS will typically vanish at that point. However, in rare cases, severe OHSS can continue to develop. Reduced success rates have been reported in fresh embryo transfers when the agonist trigger is used without hCG, so that most centers will freeze all embryos in cycles triggered only with the agonist.

In a study in rats, cross-tolerance between the benzodiazepine drug chlordiazepoxide and bretazenil has been demonstrated. In a primate study bretazenil was found to be able to replace the full agonist diazepam in diazepam dependent primates without precipitating withdrawal effects, demonstrating cross tolerance between bretazenil and benzodiazepine agonists, whereas other partial agonists precipitated a withdrawal syndrome. The differences are likely due to differences in instrinsic properties between different benzodiazepine partial agonists. Cross-tolerance has also been shown between bretazenil and full agonist benzodiazepines in rats.

Combined this evidence suggests that OCD may be associated with both increased and decreased dopamine signaling, or that a unidirectional model may not be adequate. Drug challenge studies have implicated 5-HT2A and 5-HT2A in OCD. Administration of meta- Chlorophenylpiperazine (mCPP), a non selective serotonin (5-HT) release and receptor agonist with a preference for 5-HT2C has been reported to exacerbate OCD symptoms. Psilocybin, a 5-HT2C, 5-HT2A and 5-HT1A receptor agonist has been associated with acute improvement of OCD symptoms.

Dimemebfe (5-MeO-BFE) is a recreational drug and research chemical. It acts as an agonist for the 5-HT1A and 5-HT2 family of serotonin receptors. It is related in structure to the psychedelic tryptamine derivative 5-MeO-DMT, but with the indole nitrogen replaced by oxygen, making dimemebfe a benzofuran derivative. It is several times less potent as a serotonin agonist than 5-MeO- DMT and with relatively more activity at 5-HT1A, but still shows strongest effects at the 5-HT2 family of receptors.

The affinity of an antagonist for its binding site (Ki), i.e. its ability to bind to a receptor, will determine the duration of inhibition of agonist activity. The affinity of an antagonist can be determined experimentally using Schild regression or for competitive antagonists in radioligand binding studies using the Cheng-Prusoff equation. Schild regression can be used to determine the nature of antagonism as beginning either competitive or non-competitive and Ki determination is independent of the affinity, efficacy or concentration of the agonist used.

The activity of endogenous ligands (such as the hormones estradiol and testosterone) when bound to their cognate nuclear receptors is normally to upregulate gene expression. This stimulation of gene expression by the ligand is referred to as an agonist response. The agonistic effects of endogenous hormones can also be mimicked by certain synthetic ligands, for example, the glucocorticoid receptor anti- inflammatory drug dexamethasone. Agonist ligands work by inducing a conformation of the receptor which favors coactivator binding (see upper half of the figure to the right).

Dimethandrolone (DMA), also known by its developmental code name CDB-1321, is an experimental androgen/anabolic steroid (AAS) and progestogen medication which is under investigation for potential clinical use. Dimethandrolone is an AAS, and hence is an agonist of the androgen receptor, the biological target of androgens like testosterone. It is also a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. Due to its androgenic and progestogenic activity, dimethandrolone has antigonadotropic effects.

Amylin agonist analogues slow gastric emptying and suppress glucagon. They have all the incretins actions except stimulation of insulin secretion. , pramlintide is the only clinically available amylin analogue. Like insulin, it is administered by subcutaneous injection.

In 2018 only one β3-AR agonist is approved by the European Medicines Agency (EMA) and the Food and drug Administration (FDA) as a medicine. The medicine is called Mirabegron and is used to treat OAB.

For instance, ERR-γ has been found in high concentration in the placenta, explaining reports of high bisphenol accumulation in this tissue. BPA has also been found to act as an agonist of the GPER (GPR30).

LP-211 is a drug which acts as a potent and selective agonist at the 5HT7 serotonin receptor, with better brain penetration than older 5-HT7 agonists in the same series, and similar effects in animals.

Etorphine is an extremely potent, non- selective full agonist of the μ-, δ-, and κ-opioid receptors. It also has relatively weak affinity for the nociceptin receptor. Etorphine has an LD50 of 30 μg in humans.

Quinagolide (INN, BAN; brand name Norprolac) is a selective D2 receptor agonist that is used to reduce elevated levels of prolactin (hyperprolactinemia). It has also been found to be effective in the treatment of breast pain.

In 2008, Stevens started Receptos that developed an S1P1 agonist for multiple sclerosis and inflammatory bowel disease and in 2011 he started RuiYi (now Bird Rock Bio) that developed an anti-CB1 antibody for liver fibrosis.

Sabcomeline (Memric; SB-202,026) is a selective M1 receptor partial agonist that was under development for the treatment of Alzheimer's disease. It made it to phase III clinical trials before being discontinued due to poor results.

Evocalcet (trade name Orkedia) is a drug for the treatment of hyperparathyroidism. It acts as a calcium-sensing receptor agonist. In 2018, it was approved in Japan for treatment of secondary hyperparathyroidism in patients on dialysis.

BW-723C86 is a tryptamine derivative drug which acts as a 5-HT2B receptor agonist. It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT2B receptor in a range of other tissues. BW-723C86 is actually a mixed 5-HT2B/5-HT2C agonist, and while it has good selectivity over 5-HT2A and other serotonin receptor subtypes, it is around only 3 times as selective for 2B compared to 2C and so is much less selective than most research ligands, but no superior 5-HT2B agonist was available until the potent and selective 5-HT2B activity of 6-APB was discovered in 2012. Highly selective 5-HT2C antagonists are available however, and so a combination of BW-723C86 with a selective 5-HT2C antagonist allows 5-HT2B mediated responses to be studied in isolation.

Though a pure, or silent antagonist of the under normal circumstances, bicalutamide, as well as other earlier antiandrogens like flutamide and nilutamide, have been found to possess weak partial agonist properties in the setting of overexpression and agonist activity in the case of certain mutations in the ligand-binding domain (LBD) of the . As both of these circumstances can eventually occur in prostate cancer, resistance to bicalutamide usually develops and the drug has the potential to paradoxically stimulate tumor growth when this happens. This is the mechanism of the phenomenon of antiandrogen withdrawal syndrome, where antiandrogen discontinuation paradoxically slows the rate of tumor growth. The newer drug enzalutamide has been shown not to have agonistic properties in the context of overexpression of the , though certain mutations in the can still convert it from an antagonist to agonist.

Samidorphan has been investigated for the treatment of alcoholism and cocaine addiction by its developer, Alkermes, showing similar efficacy to naltrexone but possibly with reduced side effects. However, it has attracted much more attention as part of the combination product ALKS-5461 (buprenorphine/samidorphan), where samidorphan is combined with the mixed MOR weak partial agonist and κ-opioid receptor (KOR) antagonist buprenorphine, as an antidepressant. Buprenorphine has shown antidepressant effects in some human studies, thought to be because of its antagonist effects at the KOR, but has not been further developed for this application because of its MOR agonist effects and consequent abuse potential. By combining buprenorphine with samidorphan to block the MOR agonist effects, the combination acts more like a selective KOR antagonist, and produces only antidepressant effects, without typical MOR effects such as euphoria or substance dependence being evident.

However, it acts as an agonist at the glutamatergic N-methyl-D-aspartate (NMDA) receptor site, which is important for learning and memory. Kava-kava has also attracted attention as a possible treatment, although safety concerns exist.

JTE-907 is a drug used in scientific research that acts as a selective CB2 inverse agonist. It has antiinflammatory effects in animal studies, thought to be mediated by an interaction between the CB2 receptor and IgE.

The spatial distribution of proteins is important especially upon T cell stimulation, when an immunological synapse is made, therefore this model was used in a study where the T cell was activated by a weak agonist peptide.

A small molecule agonist is GSK1702934A and antagonists are GSK417651A and GSK2293017A. A commercially available inhibitor is available in the form of a pyrazole compound, Pyr3 TRPC3 has been shown to specifically interact with TRPC1 and TRPC6.

An important mechanism of exposure therapy for anxiety disorders is extinction learning. Hofmann has shown that d-cycloserine, a partial agonist of the glutamate receptor can augment extinction learning and speed up exposure therapy of anxiety disorders.

Broxaterol is a β2 adrenoreceptor agonist. It is part of a class of drugs that affect the smooth muscle receptors in the body, often in use cases for respiratory disease that respond to this type of treatment.

The related compound 7-MeO-MiPT (cf. 5-MeO-MiPT) was also found to be inactive, suggesting that the 7-position has poor tolerance for bulky groups at this position, at least if agonist activity is desired.

Isoprenaline, or isoproterenol, is a medication used for the treatment of bradycardia (slow heart rate), heart block, and rarely for asthma. It is a non-selective β adrenoreceptor agonist that is the isopropylamine analog of epinephrine (adrenaline).

FAB-144 is an indazole-based synthetic cannabinoid that is presumed to be a potent agonist of the CB1 receptor and has been sold online as a designer drug. It is the indazole analogue of XLR-11.

This suggests that in Ca2+-dependent neuronal exocytosis synaptotagmin is a dual regulator, in absence of Ca2+ ions to inhibit SNARE dynamics, while in presence of Ca2+ ions to act as agonist in the membrane fusion process.

Alcohol Clin Exp Res, 31, 939–949.Funk, C.K. and Koob, G.F. (2007). A CRF2 agonist administered into the central nucleus of the amygdala decreases ethanol self-administration in ethanol-dependent rats. Brain Res, 1155, 172–178.

Trengestone is a progestogen, or an agonist of the progesterone receptor. It is an atypical progestogen similarly to dydrogesterone. For instance, unlike other progestogens, trengestone and dydrogesterone do not increase body temperature (i.e., have no hyperthermic effect).

O-1238 is a drug which is a cannabinoid derivative that is used in scientific research. It is a partial agonist at the cannabinoid receptor CB1, producing a maximal stimulation of 58.3% with a Ki of 8.45nM.

This caused the contractions to cease. The degree to which an opiate agonist inhibits contractions of the mouse vas deferens, and other tissues like the guinea pig ileum, is highly correlated to its potency as an analgesic.

It combines 85 mg of sumatriptan, a selective 5-hydroxytryptamine1 (5-HT1) receptor subtype agonist and 500 mg of naproxen sodium, a member of the arylacetic acid group of nonsteroidal anti- inflammatory drugs (NSAIDs), in one tablet.

RWJ-394674 is a drug that is used in scientific research. It is a potent, orally active analgesic drug that produces little respiratory depression. RWJ-394674 itself is a potent and selective agonist for δ-opioid receptors, with a Ki of 0.24 nM at δ and 72 nM at μ. However once inside the body, RWJ-394674 is dealkylated to its monodesethyl metabolite RWJ-413216, which is a potent agonist at the μ-opioid receptor and has less affinity for δ (Ki 0.26 nM at μ, 46.7 nM at δ).

JWH-176 is an analgesic drug which acts as a cannabinoid receptor agonist. Its binding affinity at the CB1 receptor is 26.0 nM, making it more potent than THC itself, however JWH-176 is particularly notable in that it is a hydrocarbon containing no heteroatoms. This demonstrates that reasonably high- affinity cannabinoid binding and agonist effects can be produced by compounds with no hydrogen bonding capacity at all, relying merely on Van der Waals interactions to bind to the receptor. It was discovered by, and named after, John W. Huffman.

The natural bile acid, chenodeoxycholic acid, was identified in 1999 as the most active physiological ligand for the farnesoid X receptor (FXR), which is involved in many physiological and pathological processes. A series of alkylated bile acid analogues were designed, studied and patented by Roberto Pellicciari and colleagues at the University of Perugia, with 6α-ethyl-chenodeoxycholic acid emerging as the most highly potent FXR agonist. FXR-dependent processes in liver and intestine were proposed as therapeutic targets in human diseases. Obeticholic acid is the first FXR agonist to be used in human drug studies.

Like other AAS, trenbolone is an agonist of the androgen receptor (AR) and hence has anabolic and androgenic activity as well as antigonadotropic activity. Trenbolone carries a rating for both anabolic potency and androgenic potency of 500, relative to a standard of nandrolone acetate (rating 100 for both). In addition to its anabolic and androgenic activity, trenbolone is an agonist of the progesterone receptor (PR), and in relation to this, has moderate to strong progestogenic activity. Conversely, trenbolone acetate is not a substrate for aromatase and hence lacks estrogenic activity.

Hypersalivation, or the excessive production of saliva, is one of the most common side effects of clozapine (30-80%). The saliva production is especially bothersome at night and first thing in the morning, as the immobility of sleep precludes the normal clearance of saliva by swallowing that occurs throughout the day. While clozapine is a muscarinic antagonist at the M1, M2, M3, and M5 receptors, clozapine is a full agonist at the M4 subset. Because M4 is highly expressed in the salivary gland, its M4 agonist activity is thought to be responsible for hypersalivation.

Allopregnanediol, or 5α-pregnane-3α,20α-diol, is an endogenous metabolite of progesterone and allopregnanolone and an isomer of pregnanediol (5β-pregnan-3α,20α-diol). It has been found to act like a partial agonist of an allosteric site of the GABA receptor and hence might play a biological role as a neurosteroid. It has also been found to act as an agonist of the human pregnane X receptor, albeit with an EC50 that is more than an order of magnitude lower than that of other endogenous pregnanes like pregnenolone, pregnanediol, allopregnanedione, and allopregnanolone.

Phantasmidine is a toxic substance derived from the Ecuadorian poisonous frog Anthony's poison arrow frog (Epipedobates Anthonyi), more commonly known as the “phantasmal poison frog”. It is a nicotinic agonist, meaning it binds to nicotinic receptors in the body and mimics the effects of the neurotransmitter acetylcholine. This causes the stimulation of the body's parasympathetic nervous system, which induces many inhibitory behaviors in the body such as decreased heart rate. Phantasmidine is characterized in the same class as epibatidine, which is a similar nicotinic acetylcholine agonist derived from a poisonous frog species.

Opioids, while commonly used in chronic neuropathic pain, are not a recommended first or second line treatment. In the short and long term they are of unclear benefit, although clinical experience suggests that opioids like tramadol may be useful for treating sudden onset severe pain In the intermediate term evidence of low quality supports utility. Several opioids, particularly levorphanol, methadone and ketobemidone, possess NMDA receptor antagonism in addition to their µ-opioid agonist properties. Methadone does so because it is a racemic mixture; only the l-isomer is a potent µ-opioid agonist.

Final maturation induction using a GnRH agonist is recommended in women with cancer undergoing fertility preservation, because ovarian hyperstimulation syndrome is associated with an increased risk of arterial thrombotic events such as stroke, myocardial infarction and peripheral arterial embolism, and this risk can add to an already increased risk caused by the cancer. Using hCG versus GnRH agonist has no effect on the risk of multiple pregnancy. Also, no difference has been found between the regimens regarding live birth rate or ongoing pregnancy rate when the controlled ovarian hyperstimulation was followed by oocyte donation.

CX614, a PAM for an AMPA receptor binding to an allosteric site and stabilizing the closed conformation Some modulators act to stabilize conformational changes associated with the agonist-bound state. This increases the probability that the receptor will be in the active conformation, but does not prevent the receptor from switching back to the inactive state. With a higher probability of remaining in the active state, the receptor will bind agonist for longer. AMPA receptors modulated by aniracetam and CX614 will deactivate slower, and facilitate more overall cation transport.

TPA-023 (MK-0777) is an anxiolytic drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. It is a subtype-selective, mixed agonist-antagonist at GABAA receptors, which acts as a partial agonist at the α2 and α3 subtypes, but as a silent antagonist at α1 and α5 subtypes. It has primarily anxiolytic and anticonvulsant effects in animal tests, but with no sedative effects even at 50 times the effective anxiolytic dose.

Studies comparing the conformational changes in helix-12 contributing to agonistic and antagonistic effects have shown an important hydrogen interaction with Glu723 residue of helix-3. At inactive state the Glu723 stabilizes conformation of helix-12 by forming a hydrogen bond to main chain amines in Met908 and Met909. When a ligand conducts an agonist effect, such as the oxime group of asoprisnil interacting with agonist binding pocket, then the hydrogen bond interaction between the previously mentioned residues in helix-12 and helix-3 strengthens, leading to docking and recruitment of coactivators.

4-Fluorophenibut (developmental code name CGP-11130; also known as β-(4-fluorophenyl)-γ-aminobutyric acid or β-(4-fluorophenyl)-GABA) is a GABAB receptor agonist which was never marketed. It is selective for the GABAB receptor over the GABAA receptor (IC50 = 1.70 μM and > 100 μM, respectively). The drug is a GABA analogue and is closely related to baclofen (β-(4-chlorophenyl)-GABA), tolibut (β-(4-methylphenyl)-GABA), and phenibut (β-phenyl-GABA). It is less potent as a GABAB receptor agonist than baclofen but more potent than phenibut.

SKF-81,297 is a synthetic drug of the benzazepine chemical class that acts as a selective dopamine D1/D5 receptor full agonist, and produces a characteristic stimulant-like pattern of anorexia, hyperactivity and self- administration in animals. This profile is shared with several related drugs such as 6-Br-APB and SKF-82,958, but not with certain other D1 full agonists such as A-77,636, reflecting functional selectivity of D1 activation. Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D1-D2 receptor heteromers.

PF-610355 (also known as PF-00610355 or PF-610,355) is an inhalable ultra- long-acting β2 adrenoreceptor agonist (ultra-LABA) that was investigated as a treatment of asthma and COPD by Pfizer. It utilizes a sulfonamide agonist headgroup, that confers high levels of intrinsic crystallinity that could relate to the acidic sulfonamide motif supporting a zwitterionic form in the solid state. Optimization of pharmacokinetic properties minimized systemic exposure following inhalation and reduced systemically-mediated adverse events. Its in vivo duration on action confirmed its potential for once-daily use in humans.

In at least certain cell types, however, TPα also stimulates cells by activating the Gs family of G proteins while TPβ also stimulates cells by activating the Gi class of G proteins. This leads to the stimulation or inhibition, respectively, of adenylate cyclase activity and thereby very different cellular responses. Differences in their C-terminal tail sequence also allow for significant differences in the two receptors internalization and thereby desensitization (i.e. loss of G protein- and therefore cell-stimulating ability) after activation by an agonist; TPβ but not TPα undergoes agonist-induced internalization.

Psilocin is the pharmacologically active agent in the body after ingestion of psilocybin or some species of psychedelic mushrooms. Psilocybin is rapidly dephosphorylated in the body to psilocin which acts as a 5-HT2A, 5-HT2C and 5-HT1A agonist or partial agonist. Psilocin exhibits functional selectivity in that it activates phospholipase A2 instead of activating phospholipase C as the endogenous ligand serotonin does. Psilocin is structurally similar to serotonin (5-HT), differing only by the hydroxyl group being on the 4-position rather than the 5 and the dimethyl groups on the nitrogen.

Milnacipran (Ixel, Savella) and its stereoisomer levomilnacipran (Fetzima) are the only widely marketed SNRIs that inhibit serotonin and norepinephrine to similar degrees, both with ratios close to 1:1. Vilazodone (Viibryd) and vortioxetine (Trintellix) are SRIs that also act as modulators of serotonin receptors and are described as serotonin modulators and stimulators (SMS). Vilazodone is a 5-HT1A receptor partial agonist while vortioxetine is a 5-HT1A receptor agonist and 5-HT3 and 5-HT7 receptor antagonist. Litoxetine (SL 81-0385) and lubazodone (YM-992, YM-35995) are similar drugs that were never marketed.

For instance, a ligand can not easily be classified as an agonist or antagonist, because it can be a little of both, depending on its preferred signal transduction pathways. Thus, such ligands must instead be classified on the basis of their individual effects in the cell, instead of being either an agonist or antagonist to a receptor. It is also important to note that these observations were made in a number of different expression systems and therefore functional selectivity is not just an epiphenomenon of one particular expression system.

Intense efforts have been carried out to design both competitive and non-competitive TRPV1 antagonists. Antagonists that bind to the agonist binding site, and lock the channel in the closed, nonconductive state are competitive antagonists. In contrast, antagonists that interact with additional binding sites on the receptor structure preventing receptor opening by the agonist or blocking its aqueous pore are non-competitive antagonists. Non-competitive antagonists acting as open channel blockers are therapeutically attractive because of their recognition of over-activated TRPV1 channels, which can reduce the potential of unwanted side effects.

Many commonly used sedative and anxiolytic drugs that affect the GABA receptor complex are not agonists. These drugs act instead as positive allosteric modulators (PAMs) and while they do bind to the GABA receptors, they bind to an allosteric site on the receptor and cannot induce a response from the neuron without an actual agonist being present. Drugs that fall into this class exert their pharmacodynamic action by increasing the effects that an agonist has when potentiation is achieved. Most general anaesthetics are PAMs of GABA-A receptor.

Positive allosteric modulators work by increasing the frequency with which the chloride channel opens when an agonist binds to its own site on the GABA receptor. The resulting increase in the concentration of Cl− ions in the postsynaptic neuron immediately hyperpolarizes this neuron, making it less excitable and thus inhibiting the possibility of an action potential. However, some general anesthetics like propofol and high doses of barbiturates may not only be positive allosteric modulators of GABA-A receptors but also direct agonists of these receptors. Alcohol is an indirect GABA agonist.

UR-AK49 is a drug used in scientific research which acts as a potent antagonist for the Neuropeptide Y / Pancreatic polypeptide receptor Y4, and also as a partial agonist at the histamine receptors H1 and H2. UR-AK49 is a pure antagonist at Y4 with no partial agonist effects, and although it is only slightly selective for Y4 over the related Y1 and Y5 receptors, as the first non-peptide Y4 antagonist developed UR-AK49 is expected to be useful in the study of this receptor and its role in the body.

Domoic acid (DA) is a neurotoxin known to cause Amnesic Shellfish Poisoning (ASP) in humans and other predators that consume contaminated aquatic organisms that have consumed P. australius. DA has been isolated in several species of red algae, but is produced mostly by members of the Pseudo-nitzschia genus. Chemical structure of domoic acid The neurotoxicity of DA is due to its classification as a glutamate receptor agonist. An agonist causes an increase in cellular function, so it prolong neurological signals after the signal should have ceased to exist.

Nepidermin (brand name Easyef), also known as recombinant human epidermal growth factor (rhEGF), is a recombinant form of human epidermal growth factor (EGF) and a cicatrizant (a drug that promotes wound healing through formation of scar tissue). It was developed by Daewoong Pharmaceutical. As a recombinant form of EGF, nepidermin is an agonist of the epidermal growth factor receptor (EGFR), and is the first EGFR agonist to be marketed. It is marketed as an ointment for the treatment of diabetic foot ulcers, wounds, and alopecia (hair loss) in Vietnam, the Philippines, Thailand, and China.

Joints are controlled by two opposing sets of muscles called extensors and flexors that must work in synchrony to allow proper and desired movement. When a muscle spindle is stretched and the stretch reflex is activated, the opposing muscle group must be inhibited to prevent from working against the agonist muscle. The spinal interneuron called Ia inhibitory interneuron is responsible for this inhibition of the antagonist muscle. The Ia afferent of the muscle spindle enters the spinal cord, and one branch synapses on to the alpha motor neuron that causes the agonist muscle to contract.

Baclofen, a GABA-B receptor agonist and antispasmodic medication, has been found to reduce cravings but without a significant benefit towards preventing relapse or improving sleep. Zolpidem, a GABA-A receptor agonist and "Z-hypnotic" medication, has shown some efficacy in treating insomnia due to cannabis withdrawal, though there is a potential for misuse. Entacapone was well tolerated and decreased cannabis cravings in a trial on a small number of patients. Topiramate, an antiepileptic drug, has shown mixed results in adolescents, reducing the volume of cannabis consumption without significantly increasing abstinence, with somewhat poor tolerability.

N-Desmethylclozapine (NDMC), or norclozapine, is a major active metabolite of the atypical antipsychotic drug clozapine. Unlike clozapine, it possesses intrinsic activity at the D2/D3 receptors, and acts as a weak partial agonist at these sites similarly to aripiprazole and bifeprunox. Notably, NDMC has also been shown to act as a potent and efficacious agonist at the M1 and δ-opioid receptors, unlike clozapine as well. It was hypothesized that on account of these unique actions, NDMC might underlie the clinical superiority of clozapine over other antipsychotics.

Levosalbutamol acts as a functional agonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges. While it is recognized that β2 adrenergic receptors are the predominant receptors on bronchial smooth muscle, data indicate that there are beta receptors in the human heart, 10–50% of which are β2 adrenergic receptors. The precise function of these receptors has not been established. However, all β adrenergic agonist drugs can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, and restlessness symptoms, and/or electrocardiographic (ECG).

Brorphine is a piperidine-based opioid analgesic compound. Some of its structural analogs, originally described in 2018, are functionally biased mu opioid receptor agonists, showing reduced side effects, especially lacking respiratory depression, when administered in high doses in mice. Importantly, however, this brominated member of the series, while it is a potent mu opioid agonist, lacks the safety margin seen for several other analogs and is not a functionally biased compound. Brorphine can instead be regarded as a typical opioid agonist, based upon its performance under various assay conditions, including robust arrestin recruitment.

LXRα and LXRβ form heterodimers with the obligate partner retinoid X receptor (RXR), which is activated by 9-cis-13,14-dihydroretinoic acid. The LXR/RXR heterodimer can be activated with either an LXR agonist (oxysterols) or a RXR agonist (9-cis-13,14-dihydroretinoic acid). Oxysterols, the oxygenated derivatives of cholesterol, such as 22(R)-hydroxycholesterol, 24(S)-hydroxycholesterol, 27-hydroxycholesterol, and cholestenoic acid, are the natural ligands for LXR. After activation, LXR binds to LXR response element (LXRE), usually a variant of the idealized sequence AGGTCAN4AGGTCA, in the promoters of LXRs' target genes.

In a mouse model of ovalbumin- induced asthma, a selective EP3 agonist reduced airway cellularity, mucus, and bronchoconstriction responses to methacholine. In this model, EP33-deficient mice, upon ovalbumin challenge, exhibited worsened allergic inflammation as measured by increased airway eosinophils, neutrophils, lymphocytes, and pro- allergic cytokines (i.e. interleukin 4, interleukin 5, and interleukin 13) as compared to wild type mice. EP3 receptor-deficient mice and/or wild type mice treated with an EP3 receptor agonist are similarly protected from allergic responses in models of allergic conjunctivitis and contact hypersensitivity.

Eyelash hypotrichosis due to the autoimmune disease, Alopecia areata, or to chemotherapy have been successfully treated with FP agonists in small Translational research studies. In a randomized, double-blind, placebo-controlled pilot study of 16 men with male pattern baldness (also termed androgenetic alopecia) topical application of the FP agonist, latanoprost, for 24 weeks produced a significant increase in scalp hair density. Despite these findings, however, a case report of one woman with female pattern hair loss found that injection of FP agonist bimatoprost failed to influence hair growth.

Morphine, the archetypal opioid, and other opioids (e.g., codeine, oxycodone, hydrocodone, dihydromorphine, pethidine) all exert a similar influence on the cerebral opioid receptor system. Buprenorphine is a partial agonist of the μ-opioid receptor, and tramadol is a serotonin norepinephrine reuptake inhibitor (SNRI) with weak μ-opioid receptor agonist properties. Tramadol is structurally closer to venlafaxine than to codeine and delivers analgesia by not only delivering "opioid-like" effects (through mild agonism of the mu receptor) but also by acting as a weak but fast-acting serotonin releasing agent and norepinephrine reuptake inhibitor.

Traditional benzodiazepines are associated with side effects such as drowsiness, physical dependence and abuse potential. It was hoped that bretazenil and other partial agonists would be an improvement on traditional benzodiazepines which are full agonists due to preclinical evidence that their side effect profile was less than that of full agonist benzodiazepines. For a variety of reasons however, bretazenil and other partial agonists such as pazinaclone and abecarnil were not clinically successful. However, research continues into other compounds with partial agonist and compounds which are selective for certain GABAA benzodiazepine receptor subtypes.

This human study also indicates that bretazenil is possibly more sedative than diazepam. The reason is unknown, but the study suggests the possibility that a full-agonist metabolite may be generated in humans but not animals previously tested or else that there are significant differences in benzodiazepine receptor population in animals and humans. In a study of monkeys bretazenil has been found to antagonize the effects of full agonist benzodiazepines. However, bretazenil has been found to enhance the effects of neurosteroids acting on the neurosteroid binding site of the GABAA receptor.

GW-405,833 (L-768,242) is a drug that acts as a potent and selective partial agonist for the cannabinoid receptor subtype CB2, with an EC50 of 0.65 nM and selectivity of around 1200x for CB2 over CB1 receptors. Animal studies have shown it to possess antiinflammatory and anti-hyperalgesic effects at low doses, followed by ataxia and analgesic effects when the dose is increased. Selective CB2 agonist drugs such as GW-405,833 are hoped to be particularly useful in the treatment of allodynia and neuropathic pain for which current treatment options are often inadequate.

Full sections in following are devoted to specific activities of gelsemine. Noted are the facts that it is a highly toxic compound, where exposure can result in paralysis and death. It is reported to be a glycine receptor agonist with significantly higher binding affinity for some of these receptors than its native agonist, glycine. In addition, it has been shown to have effects on pathways/systems in model animals (rat, rabbit), related to xenobiotic- or diet-induced oxidative stress, and in the treatment of anxiety and other conditions.

Levonorgestrel is a progestogen; that is, an agonist of the progesterone receptor (PR), the main biological target of the progestogen sex hormone progesterone. It is also a weak agonist of the androgen receptor (AR), the main biological target of the androgen sex hormone testosterone. Levonorgestrel has no other important hormonal activity, including no estrogenic, glucocorticoid, or antimineralocorticoid activity. The lack of significant mineralocorticoid or antimineralocorticoid activity with levonorgestrel is in spite of a relatively high affinity for the mineralocorticoid receptor of as much as 75% of that of aldosterone.

However, it is important that equilibrium has been reached. The effects of receptor desensitization on reaching equilibrium must also be taken into account. The affinity constant of antagonists exhibiting two or more effects, such as in competitive neuromuscular-blocking agents that also block ion channels as well as antagonising agonist binding, cannot be analyzed using Schild regression. Schild regression involves comparing the change in the dose ratio, the ratio of the EC50 of an agonist alone compared to the EC50 in the presence of a competitive antagonist as determined on a dose response curve.

BU-48 is a drug that is used in scientific research. It is from the oripavine family, related to better-known drugs such as etorphine and buprenorphine. The parent compound from which BU-48 was derived (with N-methyl rather than methylcyclopropyl on the nitrogen and lacking the aliphatic hydroxyl group) is a powerful μ-opioid agonist 1000x more potent than morphine, but in contrast BU-48 has only weak analgesic effects and instead acts primarily as a δ-opioid agonist. Its main effects are to produce convulsions, but it may also have antidepressant effects.

SERBA-2, short for selective estrogen receptor beta agonist-2, is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist. For the ERα and ERβ, SERBA-2 has affinities (Ki) of 14.5 nM and 1.54 nM, efficacies of 85% and 100%, and EC50 values of 85 nM and 3.61 nM, respectively, demonstrating 9-fold binding selectivity and 11-fold functional selectivity for the ERβ over the ERα. An enantiomer of SERBA-2, erteberel (SERBA-1), is more potent and selective in comparison and is under development for the treatment of schizophrenia.

ERA-63, also known as ORG-37663, as well as 3-methylene-7α-methyl-17α-ethynylestra-5(10)-en-17β-ol, is a synthetic, steroidal estrogen and a selective agonist of the ERα that was under development for the treatment of rheumatoid arthritis but was never marketed.Dulos, J., Hofstra, C. L., Joosten, LAB, Veening-Griffioen, D. H., Lucassen, M. A., Doorn, C. M., ... & Boots, A. M. H. (2006, July). A selective estrogen receptor alpha agonist (Org 37663) suppresses inflammation and arthritis in mouse models. In ANNALS OF THE RHEUMATIC DISEASES (Vol.

Specific A1 antagonists include 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX), and Cyclopentyltheophylline (CPT) or 8-cyclopentyl-1,3-dipropylxanthine (CPX), while specific agonists include 2-chloro-N(6)-cyclopentyladenosine (CCPA). Tecadenoson is an effective A1 adenosine agonist, as is selodenoson.

Niravoline is a chemical compound with the formula . It has diuretic and aquaretic effects and has been studied for its potential use for cerebral edema and cirrhosis. It exerts its pharmacological effect as a kappa opioid receptor agonist.

As a prokinetic agent that increases gastrointestinal motility, cisapride acts as a selective serotonin agonist in the 5-HT4 receptor subtype. Cisapride also relieves constipation-like symptoms by indirectly stimulating the release of acetylcholine in the muscarinic receptors.

Also unlike rimonabant, NESS-0327 does not appear to act as an inverse agonist at higher doses, instead being a purely neutral antagonist which blocks the CB1 receptor but does not produce any physiological effect of its own.

The molecule PBI-4050 which is an agonist of GPR40 is under investigation by the Canadian biotechnology firm Prometic. As of August 2018, it remains a promising drug targeting multiple type of fibrosis entering phase 3 clinical trials.

Although lisuride, a related drug, also binds to the 5-HT2B receptor, it acts as an antagonist rather than as an agonist. In January 2007, cabergoline (Dostinex) was reported also to be associated with valvular proliferation heart damage.

Tetrazolylglycine (Tet-Gly, LY-285,265) is a potent and selective NMDA receptor agonist, stimulating the NMDA receptor with higher potency than either glutamate or NMDA. It is a potent convulsant and excitotoxin and is used in scientific research.

Methoxyphenamine (trade names ASMI, Euspirol, Orthoxine, Ortodrinex, Proasma), also known as 2-methoxy-N-methylamphetamine (OMMA), is a β-adrenergic receptor agonist of the amphetamine class used as a bronchodilator. It acts as an anti- inflammatory in rats.

Eplivanserin is an inverse agonist on the serotonin receptor subtype 5-HT2A. In contrast to older sedating drugs acting on 5-HT2A receptors (e.g., mirtazapine, clozapine, risperidone), eplivanserin has practically no affinity to dopamine, histamine and adrenergic receptors.

He has also been involved in blues recordings with other artists as well, playing on tribute albums to Albert King and Stevie Ray Vaughan. Marino is uncle to Danny Marino, lead guitarist of Canadian metal band the Agonist.

Ballistic movement: Muscle activation and neuromuscular adaptation. Canadian Journal of Applied Physiology. 19(4): 363-378. The second agonist muscle activation is suggested to terminate the negative acceleration of the antagonist muscle contraction and thus the ballistic movement.

SSR180711 is a drug that acts as a potent and selective partial agonist for the α7 subtype of neural nicotinic acetylcholine receptors. In animal studies, it shows nootropic effects and may be useful in the treatment of schizophrenia.

Xamoterol is a cardiac stimulant. It works by binding to the β1 adrenergic receptor. It is a 3rd generation adrenergic β receptor partial agonist. It provides cardiac stimulation at rest but it acts as a blocker during exercise.

Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. Alternative splice variants of GRM8 have been described but their full-length nature has not been determined.

Estazolam is classed as a "triazolo" benzodiazepine drug. Estazolam exerts its therapeutic effects via its benzodiazepines receptor agonist properties. Estazolam at high doses decreases histamine turnover via its action at the benzodiazepine-GABA receptor complex in mouse brains.

The KOR agonist effects of oxilorphan are associated with dysphoria, which combined with its hallucinogenic effects, serve to limit its clinical usefulness; indeed, many patients who experienced these side effects refused to take additional doses in clinical trials.

DPI-287 is an opioid drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces less convulsions than most drugs from this family. It has antidepressant-like effects.

The MRGPRX receptor is a possible therapeutic target and can be pharmacologically activated using a 48/80 agonist to control bacterial infection. It is also hypothesised that other QSMs and even Gram-negative bacterial signals can activate this receptor.

Piclozotan (SUN-N4057) is a selective 5-HT1A receptor partial agonist, which has neuroprotective effects in animal studies. It has been through early clinical trials in humans for treatment of acute stroke, but results have not yet been announced.

Pilocarpus microphyllus, the Maranham Jaborandi, is a plant species in the genus Pilocarpus found native to several states in northern Brazil. Commercial production of the alkaloid muscarinic receptor agonist pilocarpine is derived entirely from the leaves of the shrub.

The activation of these receptors by an agonist as amitraz generally induces a sympathetic response. This leads to an increased heart rate, dilation of the pupils, elevation of blood pressure and blood and energy supply focus on skeletal muscles.

5F-ADB-PINACA is a cannabinoid designer drug that is an ingredient in some synthetic cannabis products. It is a potent agonist of the CB1 receptor and CB2 receptor with EC50 values of 0.24 nM and 2.1 nM respectively.

Riluzole, SKA-19, carbamazepine, and lamotrigine were capable of near complete inhibition of membrane depolarization, based on their concentration. Antillatoxin itself is an allosteric agonist for the action of batrachotoxin, and becomes even more effective when combined with brevetoxin.

Ipsapirone is a selective 5-HT1A receptor partial agonist of the piperazine and azapirone chemical classes. It has antidepressant and anxiolytic effects. Ipsapirone was studied in several placebo-controlled trials for depression and continues to be used in research.

As with psilocybin, ethocybin is rapidly dephosphorylated in the body to 4-HO-DET which then acts as a partial agonist at the 5-HT2A serotonin receptor in the brain where it mimics the effects of serotonin (5-HT).

CiclotizolamDE Patent 2445430 (WE-973) is a drug which is a thienotriazolodiazepine derivative. It is a partial agonist for the benzodiazepine site of the GABAA receptor, with similar binding affinity to related compounds like brotizolam, but a low efficacy.

CP-615,003 is a drug which acts as a subtype-selective partial agonist at GABAA receptors, and was developed by Pfizer as a potential anxiolytic; however, poor blood–brain barrier penetration make it primarily useful as a research ligand.

DHEA has been found to directly act on several neurotransmitter receptors, including acting as a positive allosteric modulator of the NMDA receptor, as a negative allosteric modulator of the GABAA receptor, and as an agonist of the σ1 receptor.

AM-694 (1-(5-fluoropentyl)-3-(2-iodobenzoyl)indole) is a designer drug that acts as a potent and selective agonist for the cannabinoid receptor CB1. It is used in scientific research for mapping the distribution of CB1 receptors.

An alternative term is serotonin partial agonist/reuptake inhibitor (SPARI), which can be applied only to vilazodone. It is similar to the marketing strategy used for the drug brexpiprazole, labeling it as a "serotonin-dopamine activity modulator" or 'SDAM'.

SR9011 is a research drug that was developed by Professor Thomas Burris of Scripps as an agonist of Rev-ErbAα with a half-maximum inhibitory concentration (IC50) = 790 nM for Rev-Erbα and IC50 = 560 nM for Rev-ErbAβ.

It has estrogenic activity, acting as a selective agonist of the ERβ, and hence is a phytoestrogen. In addition, (-)-nyasol has been found to inhibit the production of eicosanoids and nitric oxide in vitro and shows anti-inflammatory effects.

Albiglutide acts as an agonist at the GLP-1 receptor, which makes it a type of incretin mimetic. This causes an increase of insulin secretion, predominantly in the presence of high blood glucose, and also slows down gastric emptying.

Epinephrine increases the length of analgesic duration and decreases blood flow by acting as an agonist at the α1-adrenoceptor. Dexmedetomidine is not as widely used as epinephrine. Studies in humans indicate improved onset time and increased duration of analgesia.

For patients who do not respond to diet, lifestyle modification and ovulation induction, in vitro fertilisation can be performed. This usually includes controlled ovarian hyperstimulation with FSH injections, and oocyte release triggering with human chorionic gonadotropin (hCG) or a GnRH agonist.

Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic effects. It has 200 times the activity of morphine, but appears to have no addictive properties and does not depress breathing.

Sunepitron (CP-93,393) is a combined 5-HT1A receptor agonist and α2-adrenergic receptor antagonist. It was previously under development by Pfizer for the treatment of depression and anxiety. It made it to phase III clinical trials before being discontinued.

Aderis Pharmaceuticals is a privately held pharmaceutical company based in Hopkinton, Massachusetts. It was founded in 1994 to develop and commercialize pharmaceuticals. It is best known for the development of Rotigotine, a dopamine agonist made for the treatment of Parkinson's disease.

PHA-57378 is a drug which acts as an agonist at serotonin 5-HT2 receptors, having a binding affinity of 4.1 nM at the 5-HT2A subtype and 4.3 nM at 5-HT2C. It has anxiolytic effects in animal studies.

PNU-91356A (U-91356) is a drug used in scientific research which acts as a potent and reasonably selective agonist of the dopamine receptor D2, with lower affinity for the related D3 and D4 subtypes and the 5-HT1A receptor.

O-1125 (3-(1,1-dimethylhexyl-6-dimethylcarboxamide)-Δ8-tetrahydrocannabinol) is a research chemical which is a cannabinoid derivative. It has analgesic effects and is used in scientific research. It is a potent CB1 full agonist with a Ki of 1.16 nM.

Examples of ligands activating peroxisome proliferator-activated receptor gamma as partial agonists are honokiol and falcarindiol. Delta 9-tetrahydrocannabivarin (THCV) is a partial agonist at CB2 receptors and this activity might be implicated in ∆9-THCV-mediated anti-inflammatory effects.

There is some research to suggest that zafirlukast actually acts as a partial inverse agonist at the CysLT1 receptor, though zafirlukast is still classified as an antagonist at this receptor. The possible clinical significance of this effect, if true, is unknown.

16α-OHE2 is a potent ER agonist, capable of levels of cellular proliferation stimulation that near those obtained with E2. Though studies in hamster kidney tumor models showed weak carcinogenicity, the carcinogenic potential of 16α-OHE2 in humans remains unknown.

Doxanthrine is a synthetic compound which is a potent and selective full agonist for the dopamine D1 receptor. Doxanthrine has been shown to be orally active in producing contralateral rotation in the 6-hydroxy-dopamine rat model of Parkinson's disease.

Date: 7/27/2009 Using a GnRH agonist instead of hCG for inducing final oocyte maturation and/or release results in an elimination of the risk of ovarian hyperstimulation syndrome, but a slight decrease of the delivery rate of approximately 6%.

Medical treatment has not proven consistently effective. Medical regimens have included tamoxifen, progesterone, bromocriptine, the gonadotropin-releasing hormone agonist leuprorelin, and testosterone. Gestational macromastia has been treated with breast reduction drugs alone without surgery. Surgical therapy includes reduction mammaplasty and mastectomy.

The mechanism that produces the hallucinogenic and entheogenic effects of isoproscaline is most likely to result from action as a 5-HT2A serotonin receptor agonist in the brain, a mechanism of action shared by all of the hallucinogenic tryptamines and phenethylamines.

Tizanidine is an α2 receptor agonist closely related to clonidine. It has approximately one tenth to one fifteenth of the pressure lowering effect of clonidine. The relation between the α2 receptor agonism and the spasmolytic action is still not fully understood.

Benzhydrocodone is a prodrug of hydrocodone. Hydrocodone is a full agonist of the opioid receptors with a higher affinity for the mu-opioid receptor. Upon binding, hydrocodone produces an analgesic effect with no ceiling. The exact mechanism of analgesia is unknown.

Depression may also be the result of healthcare, such as with medication induced depression. Therapies associated with depression include interferon therapy, beta-blockers, isotretinoin, contraceptives, cardiac agents, anticonvulsants, antimigraine drugs, antipsychotics, and hormonal agents such as gonadotropin-releasing hormone agonist.

GSK-789,472 is a drug which acts as both a potent and selective partial agonist at the dopamine receptor D2, as well as an antagonist at the related D3 subtype, but with good selectivity over D4 and other unrelated receptors.

CJ-033466 is a drug which acts as a potent and selective 5-HT4 serotonin receptor partial agonist. In animal tests it stimulated gastrointestinal motility with 30 times the potency of cisapride, and with lower affinity for the hERG channel.

Progabide (INN; trade name Gabrene, Sanofi-Aventis) is an analogue and prodrug of γ-aminobutyric acid (GABA) used in the treatment of epilepsy. Via conversion into GABA, progabide behaves as an agonist of the GABAA, GABAB, and GABAA-ρ receptors.

Pemafibrate, marketed as Parmodia, is a peroxisome proliferator-activated receptor alpha (PPARα) agonist. It is developed and marketed by Kowa Pharmaceuticals. In 3 July 2017, Pharmaceuticals and Medical Devices Agency approved it in Japan. It is available in 0.1 mg tablets.

In addition, some cofactors bind to ER through the terminals, the DNA-binding site or other binding sites. Thus, one compound can be an ER agonist in a tissue rich in coactivators but an ER antagonist in tissues rich in corepressors.

ACC is also an exogenous partial agonist of the mammalian NMDA receptor. In 2019, the United States Environmental Protection Agency issued notice of an application for an experimental use permit to be issued for use of ACC as a pesticide.

UR-144 (TMCP-018, KM-X1, MN-001, YX-17) is a drug invented by Abbott Laboratories, that acts as a selective full agonist of the peripheral cannabinoid receptor CB2, but with much lower affinity for the psychoactive CB1 receptor.

Isoxsuprine (used as isoxsuprine hydrochloride) is a drug used as a vasodilator in humans (under the trade name Duvadilan) and equines. Isoxsuprine is a β2 adrenoreceptor agonist that causes direct relaxation of uterine and vascular smooth muscle via β2 receptors.

Ibopamine is a sympathomimetic drug, designed as a prodrug of epinine, used in ophthalmology. It induces mydriasis. It also has been investigated for use in the treatment of congestive heart failure. It acts on D1 and α receptors as an agonist.

L-655,708 (FG-8094) is a nootropic drug invented in 1996 by a team working for Merck, Sharp and Dohme, that was the first compound developed which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It acts as an inverse agonist at the α1, α2, α3 and α5 subtypes, but with much higher affinity for α5, and unlike newer α5 inverse agonists such as α5IA, L-655,708 exerts its subtype selectivity purely via higher binding affinity for this receptor subtype, with its efficacy as an inverse agonist being around the same at all the subtypes it binds to. A radiolabelled form of L-655,708 was used to map the distribution of the GABAA α5 subtype in the brain, and it was found to be expressed predominantly in the hippocampus, an area of the brain involved with learning and memory. Activation of this subtype is thought to be largely responsible for producing the cognitive side effects displayed by many benzodiazepine and nonbenzodiazepine drugs, such as amnesia and difficulties with learning and memory, and so this led researchers to conclude that a drug acting as an inverse agonist at this subtype should have the opposite effect and enhance learning and memory.

Org 28312 is a drug developed by Organon International which acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors. It was developed with the aim of finding a water-soluble cannabinoid agonist suitable for intravenous use as an analgesic, but did not proceed to human trials, with the related compound Org 28611 chosen instead due to its better penetration into the brain. The structure-activity relationships of these compounds have subsequently been investigated further leading to the development of a number of more potent analogues, derived by cyclisation around the indole or piperazine rings.

TFMPP has affinity for the 5-HT1A (Ki = 288 nM), 5-HT1B (Ki = 132 nM), 5-HT1D (Ki = 282 nM), 5-HT2A (Ki = 269 nM), and 5-HT2C (Ki = 62 nM) receptors, and functions as a full agonist at all sites except the 5-HT2A receptor, where it acts as a weak partial agonist or antagonist. Unlike the related piperazine compound meta-chlorophenylpiperazine (mCPP), TFMPP has insignificant affinity for the 5-HT3 receptor (IC50 = 2,373 nM). TFMPP also binds to the SERT (EC50 = 121 nM) and evokes the release of serotonin. It has no effects on dopamine or norepinephrine reuptake or efflux.

As a partial agonist, buprenorphine binds and activates the opioid receptors, but has only partial efficacy at the receptor relative to a full agonist, even at maximal receptor occupancy. It is thus well-suited to treat opioid dependence, as it produces milder effects on the opioid receptor with lower dependence and abuse potential. Naloxone is a pure opioid antagonist that competes with opioid molecules in the CNS and prevents them from binding to the opioid receptors. Naloxone's binding affinity is highest for the μ-opioid receptor, then the δ-opioid receptor, and lowest for the κ-opioid receptor.

When the subtype activated depends on the ligand that is bound to the GPCR, this is called functional selectivity (also known as agonist-directed trafficking, or conformation-specific agonism). However, the binding of any single particular agonist may also initiate activation of multiple different G-proteins, as it may be capable of stabilizing more than one conformation of the GPCR's GEF domain, even over the course of a single interaction. In addition, a conformation that preferably activates one isoform of Gα may activate another if the preferred is less available. Furthermore, feedback pathways may result in receptor modifications (e.g.

Induction of final maturation of oocytes is a procedure that is usually performed as part of controlled ovarian hyperstimulation to render the oocytes fully developed and thereby resulting in optimal pregnancy chances. It is basically a replacement for the luteinizing hormone (LH) surge whose effects include final maturation in natural menstrual cycles. The main medications used for induction of final maturation are human chorionic gonadotropin (hCG) and GnRH agonist. In fresh (rather than frozen) autologous cycles of in vitro fertilization, final oocyte maturation triggering with GnRH agonist instead of hCG decreases the risk of ovarian hyperstimulation syndrome but decreases live birth rate.

Levorphanol acts predominantly as an agonist of the μ-opioid receptor (MOR), but is also an agonist of the δ-opioid receptor (DOR), κ-opioid receptor (KOR), and the nociceptin receptor (NOP), as well as an NMDA receptor antagonist and a serotonin-norepinephrine reuptake inhibitor (SNRI). Levorphanol, similarly to certain other opioids, also acts as a glycine receptor antagonist and GABA receptor antagonist at very high concentrations. Levorphanol is 6 to 8 times as potent as morphine at the MOR. Relative to morphine, levorphanol lacks complete cross-tolerance and possesses greater intrinsic activity at the MOR.

MDMB-FUBINACA (also known as MDMB(N)-Bz-F and FUB-MDMB) is an indazole-based synthetic cannabinoid that is a potent agonist for the cannabinoid receptors, with Ki values of 1.14 nM at CB1 and 0.1228 nM at CB2 and EC50 values of 0.2668 nM at CB1 and 0.1411 nM at CB2, and has been sold online as a designer drug. Its benzyl analogue (instead of 4-fluorobenzyl) has been reported to be a potent agonist for the CB1 receptor (Ki = 0.14 nM, EC50 = 2.42 nM). The structure of MDMB-FUBINACA contains the amino acid 3-methylvaline or tert- leucine methyl ester.

The risk of OHSS is smaller when using GnRH antagonist protocol instead of GnRH agonist protocol for suppression of ovulation during ovarian hyperstimulation. The underlying mechanism is that, with the GnRH antagonist protocol, initial follicular recruitment and selection is undertaken by endogenous endocrine factors prior to starting the exogenous hyperstimulation, resulting in a smaller number of growing follicles when compared with the standard long GnRH agonist protocol. A Cochrane review found administration of hydroxyethyl starch decreases the incidence of severe OHSS. There was insufficient evidence to support routine cryopreservation and insufficient evidence for the relative merits of intravenous albumin versus cryopreservation.

Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on 5-HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis. This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe, as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist.

N-Arachidonoyl dopamine, an endocannabinoid found in the human CNS, structurally similar to capsaicin, activates the TRPV1 channel with an EC50 of approximately of 50 nM. N-Oleyl-dopamine, another endogenous agonist, binds to human VR1 with an Ki of 36 Nm. Another endocannabinoid anandamide has also been shown to act on TRPV1 receptors. AM404—an active metabolite of paracetamol (also known as acetaminophen) —that serves as an anandamide reuptake inhibitor and COX inhibitor also serves as a potent TRPV1 agonist. The plant-biosynthesized cannabinoid cannabidiol also shows "either direct or indirect activation" of TRPV1 receptors.

A receptor which is capable of producing a biological response in the absence of a bound ligand is said to display "constitutive activity". The constitutive activity of a receptor may be blocked by an inverse agonist. The anti-obesity drugs rimonabant and taranabant are inverse agonists at the cannabinoid CB1 receptor and though they produced significant weight loss, both were withdrawn owing to a high incidence of depression and anxiety, which are believed to relate to the inhibition of the constitutive activity of the cannabinoid receptor. The GABAA receptor has constitutive activity and conducts some basal current in the absence of an agonist.

The suppressor cells are not affected by glucosteroid response-modifying factor, so the effective setpoint for the immune cells may be even higher than the setpoint for physiological processes (reflecting leukocyte redistribution to lymph nodes, bone marrow, and skin). Rapid administration of corticosterone (the endogenous type I and type II receptor agonist) or RU28362 (a specific type II receptor agonist) to adrenalectomized animals induced changes in leukocyte distribution. Natural killer cells are affected by cortisol. Cortisol stimulates many copper enzymes (often to 50% of their total potential), including lysyl oxidase, an enzyme that cross-links collagen and elastin.

Pardoprunox (INN) (code name SLV-308) is an antiparkinsonian drug developed by Solvay for the treatment of Parkinson's disease that reached phase III clinical trials before being discontinued. It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned as well. Pardoprunox acts as a D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%). It also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity.

In drug discovery studies in order to calculate the binding affinities of the D2R ligands inside the binding domain, it's important to work on which form of D2R. It's known that the full active and inactive states are recommended to be used for the agonist and antagonist studies, respectively. Any disordering in equilibration of D2R states, which causes problems in signal transferring between the nervous systems, may lead to diverse serious disorders, such as schizophrenia, autism and Parkinson's disease. In order to control these disorders, equilibration between the D2R states is controlled by implementing of agonist and antagonist D2R ligands.

AMG-3 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is a derivative of Δ8THC substituted with a dithiolane group on the 3-position side chain. AMG-3 is a potent agonist at both CB1 and CB2 receptors with a Ki of 0.32nM at CB1 and 0.52nM at CB2, and its particularly high binding affinity has led to it being used as a template for further structural development of novel cannabinoid drugs. It has sedative and analgesic effects, with analgesia lasting for up to 36 hours after administration.

Nalfurafine (INN, USAN)Statement on a Nonproprietary Name adopted by the USAN Council (brand name Remitch; former developmental code names TRK-820, AC-820, MT-9938) is an antipruritic (anti-itch drug) that is marketed in Japan for the treatment of uremic pruritus in individuals with chronic kidney disease undergoing hemodialysis. It acts as a potent, selective, centrally-penetrant κ-opioid receptor (KOR) agonist, and is the first and currently the only selective KOR agonist to have been approved for clinical use. It has also been dubiously referred to as the "first non-narcotic opioid drug" in history.

7,8,3′-Trihydroxyflavone (7,8,3'-THF) is a flavone and small-molecule agonist of TrkB, the main receptor of brain-derived neurotrophic factor (BDNF), that was derived from 7,8-dihydroxyflavone (7,8-DHF). Relative to 7,8-DHF, 7,8,3'-THF is 2–3-fold more potent in vitro as a TrkB agonist. 7,3’-Dihydroxyflavone (7,3'-DHF) is also more potent than 7,8-DHF in vitro, indicating that a 3'-hydroxy group on the B-ring enhances TrkB agonistic activity. 7,8,3'-THF has been tested in vivo and was found to produce TrkB- dependent neuroprotective effects in mice similarly to 7,8-DHF.

Antagonism is not an intrinsic property of a particular muscle or muscle group; it is a role that a muscle plays depending on which muscle is currently the agonist. During slower joint actions that involve gravity, just as with the agonist muscle (mentioned above), the antagonist muscle can shorten and lengthen. Using the example above of the triceps brachii during a push-up, the elbow flexor muscles are the antagonists at the elbow during both the up phase and down phase of the movement. During the dumbbell curl, the elbow extensors are the antagonists for both the lifting and lowering phases.

Due to the mainly hepatic elimination, there is no risk of accumulation in people with renal impairment. One of the major active metabolites of buprenorphine is norbuprenorphine, which, in contrast to buprenorphine itself, is a full agonist of the MOR, DOR, and ORL-1, and a partial agonist at the KOR. However, relative to buprenorphine, norbuprenorphine has extremely little antinociceptive potency (1/50th that of buprenorphine), but markedly depresses respiration (10-fold more than buprenorphine). This may be explained by very poor brain penetration of norbuprenorphine due to a high affinity of the compound for P-glycoprotein.

Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) antagonist but a κ-opioid receptor (KOR) partial agonist, and has similar effects to naloxone and around the same potency as an MOR antagonist. Oxilorphan has some weak partial agonist actions at the MOR (with miosis, nausea, dizziness, and some euphoria observed) and can produce hallucinogenic/dissociative effects at sufficient doses, indicative of KOR activation. It was trialed for the treatment of opioid addiction, but was not developed commercially.

WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ. It is 100-fold selective for the ERβ over the ERα with an IC50 of 4.2 nM (compare to estradiol with IC50 values of ~3–4 nM for both the ERα and ERβ). The drug is less selective for the ERβ than is prinaberel (ERB-041, WAY-202041), another selective ERβ agonist, but is more potent in comparison. WAY-214156 may produce anti-inflammatory effects via the ERβ and has been proposed as a potential treatment for inflammatory conditions such as rheumatoid arthritis.

Homoquinolinic acid (HQA) is a potent excitotoxin which is a conformationally- restricted analogue of N-methyl-D-aspartate (NMDA) and a partial agonist of the main/glutamate site of the NMDA receptor, with some selectivity for NR2B subunit-containing receptors. It is approximately equipotent to NMDA and about five times more potent than quinolinic acid as an agonist of the NMDA receptor. HQA has also been found to label a novel, yet uncharacterized binding site, which can be distinguished from the NMDA receptor with the use of 2-carboxy-3-carboxymethylquinoline (CCMQ), a selective ligand of the uncharacterized site.

A-796,260 is a drug developed by Abbott Laboratories that acts as a potent and selective cannabinoid CB2 receptor agonist. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids with the 3-tetramethylcyclopropylmethanone group, imparts significant selectivity for CB2, and A-796,260 was found to be a highly selective CB2 agonist with little affinity for CB1, having a CB2 Ki of 4.6 nM vs 945 nM at CB1. It has potent analgesic and anti-inflammatory actions in animal models, being especially effective in models of neuropathic pain, but without producing cannabis-like behavioral effects.

UPA, a progesterone agonist-antagonist, was approved by the FDA in 2010 for use as an EC. UPA acts as a partial agonist and antagonist of the progesterone receptor and works by preventing both ovulation and fertilization. Users of UPA are likely to experience delayed menses after the expected date. In the United States, UPA is sold under the brand name Ella, which is a 30 mg single pill to be taken up to 120 hours after unprotected sex. UPA has emerged as the most effective EC pill, however, the access to UPA is very limited in US cities.

Molecular neuropharmacology involves the study of neurons and their neurochemical interactions, and receptors on neurons, with the goal of developing new drugs that will treat neurological disorders such as pain, neurodegenerative diseases, and psychological disorders (also known in this case as neuropsychopharmacology). There are a few technical words that must be defined when relating neurotransmission to receptor action: # Agonist – a molecule that binds to a receptor protein and activates that receptor # Competitive antagonist – a molecule that binds to the same site on the receptor protein as the agonist, preventing activation of the receptor # Non- competitive antagonist – a molecule that binds to a receptor protein on a different site than that of the agonist, but causes a conformational change in the protein that does not allow activation. The following neurotransmitter/receptor interactions can be affected by synthetic compounds that act as one of the three above. Sodium/potassium ion channels can also be manipulated throughout a neuron to induce inhibitory effects of action potentials.

FERb 033 is a synthetic, nonsteroidal estrogen that was synthesized in 2009 and is used in scientific research. It is a potent and selective ERβ agonist (Ki = 7.1 nM, EC50 = 4.8 nM), with 62-fold selectivity for the ERβ over the ERα.

Side effects include trouble sleeping, irritation of the nose, nausea, and headache. Long term use is not recommended due to a rhinitis medicamentosa when stopped. Use is not recommended during pregnancy. Xylometazoline is in the decongestant and alpha- adrenergic agonist families of medication.

Buprenorphine/naloxone has a milder side effect profile than methadone, and has limited respiratory effects, due to both agonist/antagonist effects. However, buprenorphine/naloxone may be less safe than methadone in people with stable liver disease, since it can elevate liver enzymes.

Schwitzer, et al., 2015 In the visual system, cannabinoids agonist induce a dose dependent modulation of calcium, chloride and potassium channels. This alters vertical transmission between photoreceptor, bipolar and ganglion cells. Altering vertical transmission in turn results in the way vision is perceived.

TMA also acts as an agonist at muscarinic receptors in post- ganglionic nerve endings in smooth muscles, cardiac muscle, and exocrine glands. In skeletal muscle, TMA initially causes fasciculations, then paralysis, as a result of the depolarization from stimulation of nicotinic ACh receptors.

The mechanism that produces the psychedelic and entactogenic effects of 2C-T-7 is most likely to result from action as a 5-HT2A serotonin receptor agonist in the brain, a mechanism of action shared by most currently-known hallucinogenic tryptamines and phenethylamines.

Aleglitazar is a peroxisome proliferator-activated receptor agonist (hence a PPAR modulator ) with affinity to PPARα and PPARγ, which was under development by Hoffmann–La Roche for the treatment of type II diabetes. It is no longer in phase III clinical trials.

Pirbuterol (trade name Maxair) is a short-acting β2 adrenoreceptor agonist with bronchodilating action used in the treatment of asthma, available (as pirbuterol acetate) as a breath-activated metered-dose inhaler. It was patented in 1971 and came into medical use in 1983.

Efficacy could be mediated through a combination of partial agonist activity D2 and 5-HT1A receptors and antagonist activity at 5-HT2A receptors. Since it is a newly approved drug by the FDA, many validation of mechanisms of action are still being studied.

AM-2201 (1-(5-fluoropentyl)-3-(1-naphthoyl)indole) is a recreational designer drug that acts as a potent but nonselective full agonist for the cannabinoid receptor. It is part of the AM series of cannabinoids discovered by Alexandros Makriyannis at Northeastern University.

Canada and many other countries prohibit manufacturers from including secondary active ingredients for the above reason; their Talwin PX does not contain naloxone. However, as a narcotic agonist–antagonist, pentazocine and its relatives can cause withdrawal in those physically dependent upon narcotics.

Dazopride (AHR-5531) is an antiemetic and gastroprokinetic agent of the benzamide class which was never marketed. It acts as a 5-HT3 receptor antagonist and 5-HT4 receptor agonist. In addition to its gastrointestinal effects, dazopride facilitates learning and memory in mice.

The music video of "Panophobia" was released October 24, 2012, and features live and behind the scenes footage of the band playing Montreal's Heavy MTL Festival. In support of Prisoners, the Agonist announced April 2013 tour dates with Danzig and Corrosion of Conformity.

BRL-52537 is a drug which acts as a potent and highly selective κ-opioid agonist. It has neuroprotective effects in animal studies, and is used for research into potential treatments for stroke and heart attack as well as more general brain research.

VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT2A. It has potent anorectic effects in animal studies.

Dexmedetomidine is a more recent agent used in this process. It is an alpha-2 adrenergic agonist that causes sedation and does have some analgesic properties. It has minimal effect on respiratory function. It will affect cardiac function as the dose increases.

Like other glutamate receptors, mGluRs have been shown to be involved in synaptic plasticity and in neurotoxicity and neuroprotection. They participate in long term potentiation and long term depression, and they are removed from the synaptic membrane in response to agonist binding.

Elafibranor (INN, code name GFT505) is an experimental medication that is being studied and developed by Genfit for the treatment of cardiometabolic diseases including diabetes, insulin resistance, dyslipidemia, and non- alcoholic fatty liver disease (NAFLD). Elafibranor is a dual PPARα/δ agonist.

TC-1698 is a drug developed by Targacept which acts as a partial agonist for the α7 subtype of neural nicotinic acetylcholine receptors. It has neuroprotective effects in animal studies, and has been used as a lead compound to find further potent derivatives.

Eclanamine (U-48,753) is a drug which was patented as an antidepressant, but was never marketed. It acts by inhibiting the reuptake of serotonin and norepinephrine. Eclanamine was discovered by accident as a derivative of the κ-opioid receptor agonist U-50,488.

Being a dual PPAR agonist, Saroglitazar (Lipaglyn) helps in controlling blood glucose and Lipid parameters especially high triglycerides and high non HDL-Cholesterol. Lipaglyn effectively reduces triglycerides and non HDL-C and controls high blood sugar, a typical situation in Insulin Resistance condition.

Naratriptan (trade names include Amerge) is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches. It is a selective 5-HT1 receptor subtype agonist. It was patented in 1987 and approved for medical use in 1997.

Tramazoline is a chemical that is used in the form of tramazoline hydrochloride in nasal decongestant preparations. It is an α-adrenergic receptor agonist that inhibits secretion of nasal mucus. It was patented in 1961 and came into medical use in 1962.

Befunolol (INN) is a beta blocker with intrinsic sympathomimetic activity used in the management of open-angle glaucoma. It also acts as a β adrenoreceptor partial agonist. Befunolol was introduced in Japan in 1983 by Kakenyaku Kako Co. under the trade name Bentos.

Preclinical and clinical data show that ospemifene is well tolerated with no major side effects. Benefits that ospemifene may have over other SERMs is its neutral effect on hot flushes and ER-agonist effect on the vagina, improving the symptoms of vaginal dryness.

Metacycline is a tetracycline antibiotic. It is used as a precursor in the industrial synthesis of doxycycline hyclate. It has been found to act as an agonist of the human pregnane X receptor ligand-binding domain and to induce CYP3A4 expression in vitro.

PF-04479745 is a research ligand developed by Pfizer. It is related to lorcaserin, and acts as a potent and selective agonist for the 5-HT2C receptor, with lower affinity and antagonist action at the related 5-HT2A and 5-HT2B receptor subtypes.

Bambuterol (INN) is a long-acting β adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline. Commercially, the AstraZeneca pharmaceutical company produces and markets bambuterol as Bambec and Oxeol. It is not available in the U.S.

A. muscaria fruitbodies contain a variable dose of muscarine, usually around 0.0003% fresh weight. This is very low and toxicity symptoms occur very rarely. Inocybe and Clitocybe contain muscarine concentrations up to 1.6%. Muscarine is a nonselective agonist of the muscarinic acetylcholine receptors.

DAA-1097 is a drug which acts as a potent and selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO, but with no affinity at central benzodiazepine receptors. It has anxiolytic effects in animal studies.

Celiprolol is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist.

FGIN-1-27 is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO. It is thought to produce anxiolytic effects by stimulating steroidogenesis of neuroactive steroids such as allopregnanolone.

EG-018 is a carbazole-based synthetic cannabinoid that has been sold online as a designer drug. It acts as a partial agonist of the CB1 and CB2 receptor, with reasonably high binding affinity, but low efficacy in terms of inducing a signaling response.

Repeated administration of receptor agonists may result in receptor internalization and/or a reduction in receptor protein signalling. The inverse agonist MK-9470 makes it possible to produce in vivo images of the distribution of CB1 receptors in the human brain with positron emission tomography.

Phantasmidine is a nicotinic agonist that acts at acetylcholine receptors. It mimics the effects of acetylcholine on the body's neuronal-based nervous systems (both the central nervous system [CNS] and the peripheral nervous system [PNS]) and the muscle-based nervous system (the somatic nervous system).

Batoprazine is a drug of the phenylpiperazine class which has been described as a serenic or antiaggressive agent. It acts as a 5-HT1A and 5-HT1B receptor agonist. It is closely related to eltoprazine, fluprazine, and naphthylpiperazine, of which possess similar actions and effects.

The mechanism of action of spinorphin has not been fully elucidated (i.e., how it acts to inhibit the enkephalinases), but it has been found to act as an antagonist of the P2X3 receptor, and as a weak partial agonist/antagonist of the FP1 receptor.

VUF-5681 is a potent and selective histamine antagonist which binds selectively to the H3 subtype. However while VUF-5681 blocks the activity of more potent H3 agonists, recent studies suggest that it may have some weak partial agonist activity when administered by itself.

Desloratadine is a selective H1-antihistamine which functions as an inverse agonist at the histamine H1 receptor. At very high doses, is also an antagonist at various subtypes of the muscarinic acetylcholine receptors. This effect is not relevant for the drug's action at therapeutic doses.

Figure 4 shows an example of a compound that fits the agonist pharmacophore perfectly. The nitrogen atom of piperazine fits the positive ionizable feature, the benzofuran part fits the aromatic ring and one hydrophobic, and the trifluoromethane part fits another hydrophobic feature of the pharmacophore.

Testing was performed on rats using this compound while characterizing various agonists of the 5-HT7 receptor. It is an agonist with a Ki value of 630.96nM. Very little other data exists about the pharmacological properties, metabolism, and toxicity of 5-MeO-pyr-T.

Product Information: TINDAMAX(R) oral tablets, tinidazole oral tablets. Mission Pharmacal Company, San Antonio, TX, 2007. The GLP-1 receptor agonist lixisenatide may slow down the absorption and activity of benznidazole, presumably due to delayed gastric emptying.Product Information: ADLYXIN(TM) subcutaneous injection, lixisenatide subcutaneous injection.

CP-809101 is a drug which acts as a potent and selective 5-HT2C receptor agonist. It had promising results in animal models of obesity and psychosis, but associated with genotoxicity which means that future use will be restricted to scientific research applications only.

Perampanel did not affect NMDA receptor currents. The extent of block (IC50, 0.56 μM) was similar at all agonist concentrations, demonstrating a noncompetitive blocking action. Parampanel did affect AMPA receptor desensitization, or the ratio of peak to late response to rapid application of AMPA.

Tazomeline (LY-287,041) is a drug which acts as a non-selective muscarinic acetylcholine receptor agonist. It was in clinical trials for the treatment of cognitive dysfunction such as that seen in Alzheimer's disease and schizophrenia, but development was apparently scrapped for unknown reasons.

Ospemifene is "an estrogen agonist/antagonist that makes vaginal tissue thicker and less fragile resulting in a reduction in the amount of pain women experience with sexual intercourse." This medication should be used for the shortest amount of time possible due to associated adverse effects.

LY-334370 is a selective 5-HT1F receptor agonist which was under development by Eli Lilly and Company for the treatment of migraine headaches. The drug showed efficacy in a phase II clinical trial but further development was halted due to toxicity detected in animals.

Dimethylphenylpiperazinium (DMPP) is a nicotinic acetylcholine receptor agonist which is selective for the ganglionic subtype. One of the earliest reports on the pharmacology of DMPP, describing it as a ganglion-stimulating, hypertensive agent, came from Graham Chen and his co-workers at Parke, Davis & Co.

Systemic absorption of the globular tetradecapeptide is minimal. Linaclotide, like the endogenous guanylin and uroguanylin it mimics, is an agonist that activates the cell surface receptor of guanylate cyclase 2C (GC-C).Linzess package insert, Allergan, plc, revised November 2015. Accessed August 18, 2016.

Androstenol and several isomers of androstanol, androstanes, are endogenous antagonists of the CAR, and despite acting as antagonists, were the basis for the naming of this receptor. More recently, dehydroepiandrosterone (DHEA), also an androstane, has been found to be an endogenous agonist of the CAR.

Binding of agonist ligands to RAR results in dissociation of corepressor and recruitment of coactivator protein that, in turn, promotes transcription of the downstream target gene into mRNA and eventually protein. In addition, the expression of RAR genes is under epigenetic regulation by promoter methylation.

AS-19 is a substance which acts as a potent agonist at the 5HT7 receptor, with an IC50 of 0.83nM. It reverses the amnesia induced by drugs such as scopolamine and dizocilpine and improves long-term memory acquisition, but inhibits short-term memory formation.

Ditolylguanidine is a sigma receptor agonist. It is somewhat selective for sigma receptors, but non-selective between the two sigma receptor subtypes, binding to both σ1 and σ2 with equal affinity. It has neuroprotective and antidepressant effects, and potentiates the effects of NMDA antagonists.

In the multiplate analyzer, anticoagulated whole blood is mixed with saline and a platelet agonist in a single-use cuvette with two pairs of electrodes. The increase in impedance between the electrodes as platelets aggregate onto them, is measured and visualized as a curve.

Physicians have experienced success treating this sleep disorder with slow-release or night-time dopaminergic drugs, and in some cases, continuous stimulation by the dopamine agonist rotigotine. Despite improved mobility during sleep, many Parkinson's patients report an extremely uncomfortable sleeping experience even after dopaminergic treatments.

RS-67,333 is a drug which has been investigated as a potential rapid-acting antidepressant, nootropic, and treatment for Alzheimer's disease. It is a high-affinity 5-HT4 receptor partial agonist, as well as a sigma receptor ligand of both subtypes to a lesser extent.

Kepone bioaccumulates in animals by factors up to a million-fold. Workers with repeated exposure suffer severe convulsions resulting from degradation of the synaptic junctions. Chronic lower level exposure causes prostate cancer. Kepone has been found to act as an agonist of the GPER (GPR30).

Chlornaltrexamine is an irreversible mixed agonist–antagonist for μ-opioid receptors, which forms a covalent bond to the active site. It is 22 times more potent than morphine. Its alkylating group is a bis(chloroalkyl)amino-residue similar to that of the nitrogen mustards.

During pregnancy, the number of oxytocin receptors increase until reaching their peak near completion of the pregnancy. An important note is that not all analogs of oxytocin work as an receptor agonist or as a uterotonic. Some may oppose uterine contractility such as atosiban.

Binding of agonist ligands (see section below) to nuclear receptors induces a conformation of the receptor that preferentially binds coactivator proteins. These proteins often have an intrinsic histone acetyltransferase (HAT) activity, which weakens the association of histones to DNA, and therefore promotes gene transcription.

It has similar actions to the triptans, acting as an agonist to the serotonin receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors. It can be used to treat acute intractable headache or withdrawal from analgesics.

The alpha-2 agonist dexmedetomidine may also be useful for agitation, but effects on heart rate and blood pressure are variable based on several studies and case reports. Lidocaine and intravenous lipid emulsion have been successfully used for serious ventricular tachyarrhythmias in several case reports.

In its pure form, dextromethorphan occurs as a white powder. Dextromethorphan is also used recreationally. When exceeding approved dosages, dextromethorphan acts as a dissociative hallucinogen. It has multiple mechanisms of action, including actions as a nonselective serotonin reuptake inhibitor and a sigma-1 receptor agonist.

V1 receptors are found in various sites around the body. The major points include the CNS, Liver, Anterior Pituitary, Muscle (both vascular and non-vascular smooth muscle), and Platelets (CLAMP). Another example of a V1 agonist is terlipressin - which is used in oesophageal varices.

Plecanatide (brand name Trulance), is a drug approved by the FDA for the treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation. Plecanatide is an agonist of guanylate cyclase-C. Plecanatide increases intestinal transit and fluid through a buildup of cGMP.

Onset of effects is around 5 hours and they last about a day. Common side effects include sleepiness. More severe side effects include red blood cell breakdown, liver problems, and allergic reactions. Methyldopa is in the alpha-2 adrenergic receptor agonist family of medication.

Its only current clinical use is in preparing patients with pheochromocytoma for surgery; its irreversible antagonism and the resultant depression in the maximum of the agonist dose-response curve are desirable in a situation where surgical manipulation of the tumour may release a large bolus of pressor amine into the circulation. Typically, phenoxybenzamine is not used in the long term, as new receptors are made to upregulate alpha stimulation. The main limiting side-effects of alpha antagonists is that the baroreceptor reflex is disrupted and thus this can cause postural hypotension. Phenoxybenzamine also has irreversible antagonist/weak partial agonist properties at the serotonin 5-HT2A receptor.

Progesterone is the most important progestogen in the body. As a potent agonist of the nuclear progesterone receptor (nPR) (with an affinity of KD = 1 nM) the resulting effects on ribosomal transcription plays a major role in regulation of female reproduction. In addition, progesterone is an agonist of the more recently discovered membrane progesterone receptors (mPRs), of which the expression has regulation effects in reproduction function (oocyte maturation, labor, and sperm motility) and cancer although additional research is required to further define the roles. It also functions as a ligand of the PGRMC1 (progesterone receptor membrane component 1) which impacts tumor progression, metabolic regulation, and viability control of nerve cells.

Metazocine is an opioid analgesic related to pentazocine. While metazocine has significant analgesic effects, mediated through a mixed agonist–antagonist action at the mu opioid receptor, its clinical use is limited by dysphoric and hallucinogenic effects which are most likely caused by activity at kappa opioid receptors (where it is a high-efficacy agonist) and/or sigma receptors. Metazocine is in Schedule II of the Controlled Substances Act 1970 of the United States as a Narcotic with ACSCN 9240 with a 19 gram aggregate manufacturing quota as of 2014. The free base conversion ratio for salts includes 0.81 for the hydrochloride and 0.74 for the hydrobromide.

5-MeO-DiBF is a psychedelic that has been sold online as a designer drug and was first definitively identified in December 2015 by a forensic laboratory in Slovenia. It is thought to act as an agonist for the 5-HT1A and 5-HT2 family of serotonin receptors. It is related in structure to the psychedelic tryptamine derivative 5-MeO-DiPT, but with the indole nitrogen replaced by oxygen, making 5-MeO-DiBF a benzofuran derivative. It is several times less potent as a serotonin agonist than 5-MeO-DiPT and with relatively more activity at 5-HT1A, but still shows strongest effects at the 5-HT2 family of receptors.

Buspirone/testosterone (tentative brand name Lybridos) is a combination of buspirone, a 5-HT1A receptor partial agonist, α2-adrenergic receptor antagonist, and D2 autoreceptor antagonist, and testosterone, an androgen or androgen receptor agonist, which is under development by the pharmaceutical company Emotional Brain for the treatment of female sexual dysfunction. Both buspirone and testosterone have individually been found to be effective in the treatment of female sexual dysfunction in clinical studies, and so their combination could be anticipated to be even more effective. As of January 2016, the combination is in phase II clinical trials, with a phase III trial being planned in the United States and Europe.

Bionovo’s lead drug candidate, Menerba (formerly known as MF101), is a novel selective estrogen receptor beta (ERβ) agonist designed to treat vasomotor symptoms (hot flashes) associated with menopause. Although Menerba is a selective estrogen receptor modulator (SERM), it is distinct from the other FDA-approved SERMs, such as tamoxifen and raloxifene, since these drugs have mixed agonist/antagonist activity and are not selective in transcriptional regulation to one of the two known estrogen receptor subtypes. Menerba completed its Phase II clinical trial, showing the drug to be safe, clinically efficacious and well tolerated. The drug will begin its Phase III clinical trial pending FDA approval.

Thienorphine is a very potent, extremely long-acting, orally-active opioid analgesic with mixed agonist–antagonist properties which was developed by the Beijing Institute of Pharmacology and Toxicology as a potential treatment for opioid dependence. It is a high-affinity, balanced ligand of the μ- (Ki = 0.22 nM), δ- (Ki = 0.69 nM), and κ-opioid receptors (Ki = 0.14 nM), behaving as a partial agonist of the μ- (Emax = 19%–28%) and κ-opioid receptors (Emax = 65–75%) and as an antagonist of the δ-opioid receptor. It also possesses relatively low affinity for the nociceptin receptor (Ki = 36.5 nM), where it acts as an antagonist.

Comparison of SSRIs and the 5-HT2C receptor agonists showed that the agonists decreased immobility time and increased swimming time in the FST (forced swim test) in rats in a manner comparable to SSRIs. In the 1990s 5-HT2C receptors have received more attention as many studies have shown that selective 5-HT2C receptor agonists may be more suited in the treatment for psychotic indications. A 5-HT2C agonist may be expected to reduce positive symptoms of schizophrenia by reducing dopamine release in the mesolimbic dopamine pathway. Vabicaserin (SCA-136) is a 5-HT2C agonist that has shown promise in preliminary testing for the treatment of schizophrenia.

Along with the other inhibitory neurosteroids, allopregnanolone appears to have little or no action at other ligand-gated ion channels, including the NMDA, AMPA, kainate, and glycine receptors. Unlike progesterone, allopregnanolone is inactive at the classical nuclear progesterone receptor (PR). However, allopregnanolone can be intracellularly oxidized into 5α-dihydroprogesterone, which does act as an agonist of the PR, and for this reason, allopregnanolone can produce PR-mediated progestogenic effects. In addition, allopregnanolone was reported in 2012 to be an agonist of the membrane progesterone receptors (mPRs) discovered shortly before, including mPRδ, mPRα, and mPRβ, with its activity at these receptors about a magnitude more potent than at the GABAA receptor.

A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the mu opioid receptor show equivalent efficacy for treating pain with reduced risk for addictive potential and respiratory depression. Studies within the chemokine receptor system also suggest that GPCR biased agonism is physiologically relevant. For example, a beta-arrestin biased agonist of the chemokine receptor CXCR3 induced greater chemotaxis of T cells relative to a G protein biased agonist.

The primary challenges of developing serotnergic/antiserotonergic ergolines is attributed to serotonin, or 5-HT, acting on various distinct receptor sites. Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, such as metergoline, a 5-HT1A agonist/5-HT2A antagonist, and mesulergine, a 5-HT2A/2C antagonist. The selectivity and affinity of ergolines for certain 5-HT receptors can be improved by introducing a bulky group on the phenyl ring of the ergoline skeleton, which would prevent the interaction of ergoline derivatives with receptors. This methodology has been used to develop selective 5-HT1A and 5-HT2A ergolines in particular.

Desmethylzopiclone has been found to have partial agonist properties, unlike the parent drug zopiclone, which is a full agonist. The mechanism of action of zopiclone is similar to benzodiazepines, with similar effects on locomotor activity and on dopamine and serotonin turnover. A meta-analysis of randomised controlled clinical trials that compared benzodiazepines to zopiclone or other Z drugs such as zolpidem and zaleplon has found few clear and consistent differences between zopiclone and the benzodiazepines in sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia, and daytime alertness. Zopiclone is in the cyclopyrrolone family of drugs.

Clonidine treats high blood pressure by stimulating α2 receptors in the brain stem, which decreases peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding has a sympatholytic effect, suppresses release of norepinephrine, ATP, renin, and neuropeptide Y which if released would increase vascular resistance. Clonidine also acts as an agonist at imidazoline-1 (I1) receptors in the brain, and it is hypothesized that this effect may contribute to reducing blood pressure by reducing signaling in the sympathetic nervous system, but this effect acts upstream of the central α2 agonist effect of clonidine.

AM-919 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid receptor agonist. It is a derivative of HU-210 which has been substituted with a 6β-(3-hydroxypropyl) group. This adds a "southern" aliphatic hydroxyl group to the molecule as seen in the CP-series of nonclassical cannabinoid drugs, and so AM-919 represents a hybrid structure between the classical dibenzopyran and nonclassical cannabinoid families. AM-919 is somewhat less potent than HU-210 itself, but is still a potent agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 2.2 nM at CB1 and 3.4 nM at CB2.

Levallorphan was also used in combination with opioid analgesics to reduce their side effects, mainly in obstetrics, and a very small dose of levallorphan used alongside a full agonist of the MOR can produce greater analgesia than when the latter is used by itself. The combination of levallorphan with pethidine (meperidine) was indeed used so frequently, a standardized formulation was made available, known as Pethilorfan. As an agonist of the KOR, levallorphan can produce severe mental reactions at sufficient doses including hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety, confusion, dizziness, disorientation, derealization, feelings of drunkenness, delusions, paranoia, and bizarre, unusual, or disturbing dreams.

The term SERM was introduced to describe these compounds that have a combination of estrogen agonist, partial agonist, or antagonist activities depending on the tissue. Toremifene has been shown to be compatible with tamoxifen, and in 1996 it was approved for use in the treatment of breast cancer in postmenopausal women. Raloxifene originally failed as a breast cancer drug due to its poor performance in comparison to tamoxifen in the laboratory but the estrogenic effects of raloxifene on bone led to its rediscovery and approval in 1997. It was approved for prevention and treatment of osteoporosis and was the first clinically available SERM to prevent both osteoporosis and breast cancer.

This alignment contributes to the hydrogen bonding between the nitrogen in the sulfonamine and the Ser138 in the binding site. It is also favorable to the formation of the hydrogen bond between the oxygen of the sulfonamine and Thr202. Other binding in the pocket of the binding site occurs with the nitrogen atom in the pentene ring of the indole structure of the triptan and the amino acid Ser352. This energetically favorable position of the agonist makes it possible for additional binding of the ligand to other Ser in the binding site, along with additional anchoring between Phe in the pocket of the binding site and the indole of the agonist.

A washout step in the assay will usually distinguish between non-competitive and irreversible antagonist drugs, as effects of non-competitive antagonists are reversible and activity of agonist will be restored. Irreversible competitive antagonists also involve competition between the agonist and antagonist of the receptor, but the rate of covalent bonding differs and depends on affinity and reactivity of the antagonist. For some antagonist, there may be a distinct period during which they behave competitively (regardless of basal efficacy), and freely associate to and dissociate from the receptor, determined by receptor-ligand kinetics. But, once irreversible bonding has taken place, the receptor is deactivated and degraded.

A follow-up analysis for ganirelix done by the Marketing Authorisation Holder compared the number of congenital malformations between individuals whose mothers were treated with ganirelix compared with individuals whose mothers were treated with a GnRH agonist. The total number of congenital malformations was higher in the ganirelix group than in the GnRH agonist group (7.6% vs. 5.5%). This falls within the range for the normal incidence of congenital malformations, and current data do not suggest that ganirelix increases the incidence of congenital malformations or anomalies. No important differences in the frequency of ectopic pregnancies and miscarriage were noted with the use of ganirelix.

Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is a novel analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes. It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose. Human trials showed little potential for development of dependence or abuse, and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief.

The substitution of certain bulky groups on nitrogen 17 converts an opioid agonist into an opioid antagonist, the most important of which is naloxone, a non-selective opioid antagonist with no opioid agonist properties whatsoever ("silent" antagonist). Additionally, substitution of certain very bulky groups on carbon 6 converts naloxone into a peripherally-selective opioid antagonist with no centrally- selective antagonist properties (naloxegol). The addition of a two-carbon bridge between carbons 6 and 14 (e.g., 6,14-ethano, or 6,14-etheno), and which significantly distorts the C ring, may increase potency 1,000 to 10,000 times, or greater, compared to morphine, as in etorphine, and others.

Embryo cryopreservation is generally performed as a component of in vitro fertilization (which generally also includes ovarian hyperstimulation, egg retrieval and embryo transfer). The ovarian hyperstimulation is preferably done by using a GnRH agonist rather than human chorionic gonadotrophin (hCG) for final oocyte maturation, since it decreases the risk of ovarian hyperstimulation syndrome with no evidence of a difference in live birth rate (in contrast to fresh cycles where usage of GnRH agonist has a lower live birth rate). The main techniques used for embryo cryopreservation are vitrification versus slow programmable freezing (SPF). Studies indicate that vitrification is superior or equal to SPF in terms of survival and implantation rates.

The partial agonist of VGSC Hoiamide A and B may be able to mimic activity-dependent control of neuronal development through the up-regulation of pathways that influence neuronal growth and plasticity. Hoiamide D is a molecule that may applications as a precursor molecule for cancer therapies.

They are also being studied in the treatment of breast cancer. Examples of antiprogestogens include the progesterone receptor weak partial agonist mifepristone, the selective progesterone receptor modulator (SPRM) ulipristal acetate, and the silent antagonist aglepristone. For medical abortion, mifepristone is combined with a prostaglandin (e.g., gemeprost).

Agatolimod (also known as CpG 7909, ODN 2006, PF-3512676, VaxImmune, and ProMuneT) is a CpG Oligodeoxynucleotide which acts as a toll-like receptor 9 agonist. Agatolimod stimulates the immune system and has been tested for prevention and treatment of cancer, infectious diseases, allergies, and asthma.

2-Hydroxyestradiol has been identified as a prodrug of 2-methoxyestradiol, a transformation which is very efficiently catalyzed by catechol O-methyltransferase in the liver. 2-Methoxyestradiol is not estrogenic but is a potent angiogenesis inhibitor and agonist of the GPER with potential therapeutic implications in cancer.

A-349,821 is a potent and selective histamine H3 receptor antagonist (or possibly an inverse agonist). It has nootropic effects in animal studies, although there do not appear to be any plans for clinical development at present and it is currently only used in laboratory research.

Remifentanil is a specific μ-receptor agonist. Hence, it causes a reduction in sympathetic nervous system tone, respiratory depression and analgesia. The drug's effects include a dose-dependent decrease in heart rate and arterial pressure and respiratory rate and tidal volume. Muscle rigidity is sometimes noted.

Tolgabide (INN; development code SL-81.0142) is a drug which was patented by Synthélabo as an anticonvulsant but was never marketed. It is an analogue of progabide and acts similarly to it as a prodrug of GABA, and therefore as an indirect agonist of the GABA receptors.

THJ-2201 is an indazole-based synthetic cannabinoid that presumably acts as a potent agonist of the CB1 receptor and has been sold online as a designer drug. It is a structural analog of AM-2201 in which the central indole ring has been replaced by indazole.

Phenethylamine, being similar to amphetamine in its action at their common biomolecular targets, releases norepinephrine and dopamine. Phenethylamine also appears to induce acetylcholine release via a glutamate-mediated mechanism. Phenethylamine has been shown to bind to human trace amine-associated receptor 1 (hTAAR1) as an agonist.

Bay K8644 is a chemical compound that functions as a calcium channel agonist. Bay K8644 is used primarily as a biochemical research tool for this effect. It is a structural analog of nifedipine with positive inotropic activity, and as an aromatic it is highly lipid soluble.

NESS-040C5 is a potent cannabinoid agonist which was developed for the treatment of glaucoma.Paolo Lazzari et al. Pharmaceutical Compounds. US Patent 8106218 It has reasonable selectivity for the CB2 receptor subtype, having a CB2 affinity of 0.4nM, and 25x selectivity over the related CB1 receptor.

Aclidinium bromide/formoterol, sold under the brand names Duaklir and Brimica, is a fixed-dose combination medication for inhalation, used in the management of chronic obstructive pulmonary disease (COPD). It consists of aclidinium bromide, a long-acting muscarinic antagonist, and formoterol, a long-acting β2 agonist.

Cinitapride (trade names Cintapro, Pemix) is a gastroprokinetic agent and antiulcer agent of the benzamide class which is marketed in India, Mexico, Pakistan and Spain. It acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors.

Stress, cold weather, and infections lead to an increase in symptoms, and sleep decreases them. SPS patients suffer superimposed spasms and extreme sensitivity to touch and sound. These spasms primarily occur in the proximal limb and axial muscles. There are co-contractions of agonist and antagonist muscles.

Although originally thought to act as a direct agonist of adrenergic receptors, PPA was subsequently found to show only weak or negligible affinity for these receptors, and has been instead characterized as an indirect sympathomimetic which acts by inducing norepinephrine release and thereby activating adrenergic receptors.

ICI-204,448 is a drug which acts as a potent and peripherally selective κ-opioid agonist, with possible uses in the treatment of heart attack as well as anti-itching effects. It is used in research to distinguish centrally from peripherally mediated kappa opioid receptor effects.

So, harmine and harmaline are reversible selective inhibitors of monoamine oxidase-A. Reserpine reduces concentration of monoamines in presynaptic and synaptic neurons, thereby inducing antihypertensive and antipsychotic effects. Some indole alkaloids interact with other types of receptors. Mitragynine is an agonist of the μ-opioid receptor.

PHA-543,613 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.

It is also implicated in the generation and maintenance of REM sleep. In animal studies, lesions of the pontine tegmentum greatly reduce or even eliminate REM sleep. Injection of a cholinergic agonist (e.g. carbachol), into the pontine tegmentum produces a state of REM sleep in cats.

Labetalol possesses intrinsic sympathomimetic activity. In particular, it is a partial agonist at beta2- receptors located in the vascular smooth muscle. Labetalol relaxes vascular smooth muscle by a combination of this partial beta2- agonism and through alpha1- blockade. Overall, this vasodilatory effect can decrease blood pressure.

MDMB-CHMICA acts as a highly potent full agonist of the CB1 receptor with an efficacy of 94% and an EC50 value of 0.14 nM, which is approximately 8 times lower than the EC50 of JWH-018 (1.13 nM) and twofold lower than AB-CHMINACA (0.27 nM).

Nemonapride (エミレース, Emilace (JP)) is an atypical antipsychotic approved in Japan for the treatment of schizophrenia. It was launched by Yamanouchi in 1991. Nemonapride acts as a D2 and D3 receptor antagonist, and is also a potent 5-HT1A receptor agonist. It has affinity for sigma receptors.

Serious side effects may include pathological gambling, low blood pressure with standing and hallucinations. Use in pregnancy and breastfeeding is of unclear safety. It is a dopamine agonist and works by triggering dopamine D2 receptors. It was approved for medical use in the United States in 1997.

FG-7142 (ZK-31906) is a drug which acts as a partial inverse agonist at the benzodiazepine allosteric site of the GABAA receptor. It has anorectic, anxiogenic and pro-convulsant effects. It also increases release of acetylcholine and noradrenaline, and improves memory retention in animal studies.

6-Hydroxymelatonin (6-OHM) is a naturally occurring, endogenous, major active metabolite of melatonin. Similar to melatonin, 6-OHM is a full agonist of the MT1 and MT2 receptors. It is also an antioxidant and neuroprotective, and is even more potent in this regard relative to melatonin.

Drotebanol (Oxymethebanol) is a morphinan derivative that acts as an opioid agonist. It was invented by Sankyo Company in Japan during the 1970s. It is synthesised from thebaine. Drotebanol has powerful antitussive (cough suppressant) effects, and is around 10x more potent than codeine in producing this effect.

Tulobuterol (INN) is a long-acting beta2-adrenergic receptor agonist, marketed in Japan as a transdermal patch under the name Hokunalin tape (ホクナリンテープ). Currently, it is only legal in 7 countries: Japan, Germany, China, South Korea, Bangladesh, Pakistan, and Venezuela. It is available in India also.

Methylergometrine is contraindicated in patients with hypertension and pre- eclampsia. It is also contraindicated in HIV positive patients taking protease inhibitors, delavirdine and efavirenz (which is also an agonist at the 5HT2A-mGlu2 receptor protomer and increases the chances of a patient experiencing hallucinations during methylergometrine therapy).

Zearalenone is heat-stable and is found worldwide in a number of cereal crops, such as maize, barley, oats, wheat, rice, and sorghum. In addition to its actions on the classical estrogen receptors, zearalenone has been found to act as an agonist of the GPER (GPR30).

CUMYL-THPINACA (also known as SGT-42) is an indazole-3-carboxamide based synthetic cannabinoid. CUMYL-THPINACA acts as a potent agonist for the cannabinoid receptors, with approximately 6x selectivity for CB1, having an EC50 of 0.1nM for human CB1 receptors and 0.59nM for human CB2 receptors.

CUMYL-PINACA (also known as SGT-24) is an indazole-3-carboxamide based synthetic cannabinoid. CUMYL-PINACA acts as a potent agonist for the cannabinoid receptors, with approximately 3x selectivity for CB1, having an EC50 of 0.15nM for human CB1 receptors and 0.41nM for human CB2 receptors.

DCG-IV is a research drug which acts as a group-selective agonist for the group II metabotropic glutamate receptors (mGluR2/3). It has potent neuroprotective and anticonvulsant effects in animal studies, as well as showing anti-Parkinsonian effects, but also impairs the formation of memories.

Basmisanil (; developmental codes RG-1662 and RO5186582) is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome. As of June 2016, it is no longer studied.

Anabaseine (3,4,5,6-Tetrahydro-2,3’-bipyridine) is an alkaloid toxin produced by Nemertines and Aphaenogaster ants. It is structurally similar to nicotine and anabasine. Similarly, it has been shown to act as an agonist on most nicotinic acetylcholine receptors in the central nervous system and peripheral nervous system.

H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of protein kinase A. PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine H2 receptor agonist.

Buserelin was first described in 1976 and was introduced for medical use in 1984. Intranasal buserelin was the first GnRH agonist demonstrated to achieve medical castration in humans. This was initially observed via a marked decrease in circulating testosterone levels in a single patient in 1980.

Riligustilide is a nonsteroidal phytoprogestogen that is found in Ligusticum chuanxiong. It is a very weak agonist of the progesterone receptor (EC50 ≈ 81 μM). Another compound in the plant, 3,8-dihydrodiligustilide, is also a phytoprogestogen, but is almost 1,000-fold more potent in comparison (EC50 = 90 nM).

Herkinorin is an opioid analgesic that is an analogue of the natural product Salvinorin A. It was discovered in 2005 during structure-activity relationship studies into neoclerodane diterpenes, the family of chemical compounds of which Salvinorin A is a member. Unlike Salvinorin A which is a selective κ-opioid agonist with no significant μ-opioid receptor affinity, herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A. Herkinorin is a semi-synthetic compound, made from Salvinorin B, which is most conveniently made from Salvinorin A by deacetylation, as while both Salvinorin A and Salvinorin B are found in the plant Salvia divinorum, Salvinorin A is present in larger quantities. A study in primates showed it to act as both a peripherally active μ and κ agonist with a fast onset of action. The study did not find any evidence of central activity in primates and questions whether herkinorin's effects are due entirely to peripheral binding.

It is also a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. Due to its progestogenic activity, oxendolone has antigonadotropic effects. Oxendolone has no other important hormonal activity. Oxendolone was introduced for medical use in 1981.

Modafinil and armodafinil each act as a selective, weak, atypical dopamine reuptake inhibitor (DRI) whereas adrafinil acts as a prodrug for modafinil. Other eugeroics include solriamfetol, which acts as a norepinephrine–dopamine reuptake inhibitor (NDRI), and pitolisant, which acts as a histamine 3 (H₃) receptor antagonist/inverse agonist.

2-Methoxyestradiol is derived from estradiol, although it interacts poorly with the estrogen receptors (2,000-fold lower activational potency relative to estradiol). However, it retains activity as a high- affinity agonist of the G protein-coupled estrogen receptor (GPER) (10 nM, relative to 3–6 nM for estradiol).

Repinotan HCI (BAYx3702) acts as a highly selective 5-HT1A receptor full agonist. It is blocked by the specific 5-HT1A receptor antagonist, WAY 100135 and its primary metabolizer is CYP2D6. Ethnic differences are known to have an effect on CYP2D6. Repinotan is believed to operate through neuronal hyperpolarization.

While each joint is commonly understood as having an agonist-antagonist pair, not all joint movement is controlled locally. Finally, movement kinematics are not identical even when performing the same motion repeatedly; natural variation in position, velocity, and acceleration of the limb occur even during seemingly identical movements.

Prasad V. Bharatam is Professor of Medicinal Chemistry at National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, India. His area of research include Quantum Medicinal Chemistry, Pharmacoinformatics, synthesis of computationally designed molecules (anti-diabetic belonging to class PPAR-γ agonist and biguanides), drug delivery using dendrimers.

Results from cerebellar cortical inactivation studies are similar to those reported for lesion studies. For example, Krupa (1993) inactivated lobule HVI with the GABAA receptor agonist Muscimol and found significant acquisition deficits, but animals eventually learned. Clark et al. (1997) replicated these results with a cooling probe in HVI.

300x300pxAtipamezole is a competitive antagonist at ɑ2-adrenergic receptors that competes with dexmedetomidine, an ɑ2-adrenergic receptors agonist. It does not directly interact with dexmedetomidine; rather, their structural similarity allows atipamezole to easily compete for receptor binding sites. Atipamezole reverses analgesia by blocking norepinephrine feedback inhibition on nociceptors.

N6-Cyclopentyladenosine (CPA) is a drug which acts as a selective adenosine A1 receptor agonist. It has mainly cardiovascular effects with only subtle alterations of behavior. CPA is widely used in scientific research into the adenosine receptors and has been used to derive a large family of derivatives.

HZ-2 is a drug which acts as a highly selective κ-opioid agonist. It is a potent analgesic with around the same potency as morphine, with a long duration of action and high oral bioavailability. Side effects include sedation, nausea and dysphoria as well as diuretic effects.

U-92,016-A is a psychoactive drug and research chemical used in scientific studies. It acts as a potent, high efficacy, and selective 5-HT1A receptor full agonist with a long duration of action. It has been suggested that it could be developed as an anxiolytic or antidepressant drug.

SB-243213 is a research chemical which acts as a selective inverse agonist for the 5HT2C receptor and has anxiolytic effects. It has better than 100x selectivity for 5-HT2C over all other receptor subtypes tested, and a longer duration of action compared to older 5-HT2C antagonist ligands.

Serious side effects may include an urge to gamble or have sex, heart failure, and low blood pressure. Use in pregnancy and breastfeeding is of unclear safety. It is a dopamine agonist of the non-ergoline class. Pramipexole was approved for medical use in the United States in 1997.

12-(S)-hydroxy-5Z,8E,10E-heptadecatrienoic acid or 12-HHT) and agonist of Leukotriene B4 receptors (i.e. BLT2 receptors) and mediator of certain BLT2 receptor actions.J Biochem. 2015 Feb;157(2):65-71 The enzyme plays a role in several pathophysiological processes including hemostasis, cardiovascular disease, and stroke.

Bromocriptine (originally marketed as Parlodel, subsequently under many names) is an ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes. It was patented in 1968 and approved for medical use in 1975.

Xylazine is an analogue of clonidine and an agonist at the α2 class of adrenergic receptor. It is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals.Xylazine at drugs.com Veterinarians also use xylazine as an emetic, especially in cats.

Oxidative damage is accelerated at high light intensity. Atrazine's effects in humans and animals primarily involve the endocrine system. Studies suggest that atrazine is an endocrine disruptor that can cause hormone imbalance. Atrazine has been found to act as an agonist of the G protein-coupled estrogen receptor 1.

Opioids inhibit the firing of neurons in the locus coeruleus. When opioid consumption is stopped, the increased activity of the locus coeruleus contributes to the symptoms of opiate withdrawal. The alpha2 adrenoceptor agonist clonidine is used to counteract this withdrawal effect by decreasing adrenergic neurotransmission from the locus coeruleus.

Although the compound is hazardous, it is used in chemical industry as a precursor to trovafloxacin. Procedures for safe industrial handling have been published. Another location where EDA was used is in the production of BI-4752, a recently invented 5HT2C agonist that is even superior to lorcaserin.

PHCCC is a research drug which acts as a glutamate receptor ligand, particularly being a positive allosteric modulator at the mGluR4 subtype, as well as an agonist at mGluR6. It has anxiolytic effects in animal studies. PHCCC and similar drugs have been suggested as novel treatments for Parkinson's disease.

Improvements were found in the areas of the body that expressed GLP-1R. In addition to its other effects on the Huntington's disease mouse model, daily treatment of Ex-4, the GLP-1R agonist, significantly delayed the onset of mortality and extended the lifespan by approximately one month.

Found in numerous species of mint, (including peppermint, spearmint, and watermint), the naturally-occurring compound menthol is a weak KOR agonist owing to its antinociceptive, or pain blocking, effects in rats. In addition, mints can desensitize a region through the activation of TRPM8 receptors (the 'cold'/menthol receptor).

A nonsteroidal diphenylacrylamide derivative, STX, which is structurally related to 4-hydroxytamoxifen (afimoxifene), is an agonist of the receptor with greater potency than estradiol (20-fold higher affinity) that has been discovered. Fulvestrant (ICI-182,780) has been identified as an antagonist of Gq-mER, but is not selective.

Sucralfate has a similar effectiveness to H2 receptor blockers; however, sucralfate needs to be taken multiple times a day, thus limiting its use. Baclofen, an agonist of the GABAB receptor, while effective, has similar issues of needing frequent dosing in addition to greater adverse effects compared to other medications.

Hexoprenaline is a selective β2 adrenergic receptor agonist used in the treatment of asthma. Hexoprenaline is also used in some countries (such as Russia and Switzerland) as a tocolytic agent (i.e., labor suppressant), with the most common trade name being Gynipral. It is not approved by U.S. FDA.

Zalospirone (WY-47,846) is a selective 5-HT1A partial agonist of the azapirone chemical class. It was found to be effective in the treatment of anxiety and depression in clinical trials, but a high proportion of subjects dropped out due to side effects and development was subsequently never completed.

Proceedings of the National Academy of Sciences USA. 2003 Sep 16;100(19):11086-91. Baldi E, Bucherelli C, Schunack W, Cenni G, Blandina P, Passani MB. The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat. Neuropharmacology. 2005 Feb;48(2):246-51.

Table 2: Microbial metabolites: their synthesis, mechanisms of action, and effects on health and disease Figure 1: Molecular mechanisms of action of indole and its metabolites on host physiology and disease The amber-woody fragrance timberol antagonizes this activity of trimethylamine. 3-Iodothyronamine is an inverse agonist of hTAAR5.

Secondary amenorrhea's most common and most easily diagnosable causes are pregnancy, thyroid disease, and hyperprolactinemia. A pregnancy test is a common first step for diagnosis. Hyperprolactinemia, characterized by high levels of the hormone prolactin, is often associated with a pituitary tumor. A dopamine agonist can often help relieve symptoms.

While the exact function of C6orf222 remains unknown, there has been evidence for it being involved in apoptosis as a pro-apoptotic protein due to the conserved BH3 interacting domain death agonist located at the C-terminus of the protein between amino acid residues 535 to 611 in humans.

Although there are studies which indicate the disease prevention (cardio-protective and hormone associated cancers like breast cancer) benefits of lignans, the results are not yet conclusive.Linus Pauling Institute at Oregon State University Matairesinol has been found to act as an agonist of the adiponectin receptor 1 (AdipoR1).

WAY-267464 is a potent, selective, non-peptide agonist for the oxytocin receptor, with negligible affinity for the vasopressin receptors. Contradictorily however, though originally described as selective for the oxytocin receptor and lacking affinity for the vasopressin receptors, it has since been reported to also act as a potent vasopressin V1A receptor antagonist (in contrast to oxytocin, which is a weak agonist of the V1A receptor). WAY-267464 has been shown to cross the blood-brain-barrier to a significantly greater extent than exogenously applied oxytocin, and in animal tests produces centrally-mediated oxytocinergic actions such as anxiolytic effects, but with no antidepressant effect evident. It was developed by a team at Ferring Pharmaceuticals.

Orciprenaline, also known as metaproterenol, is a bronchodilator used in the treatment of asthma. Orciprenaline is a moderately selective β2 adrenergic receptor agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle, with minimal or no effect on α adrenergic receptors. The pharmacologic effects of β adrenergic agonist drugs, such as orciprenaline, are at least in part attributable to stimulation through β adrenergic receptors of intracellular adenylyl cyclase, the enzyme which catalyzes the conversion of ATP to cAMP. Increased cAMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from many cells, especially from mast cells.

Fexaramine is an investigational compound which acts as an agonist of the farnesoid X receptor (FXR), which is a bile acid-activated nuclear receptor that controls bile-acid synthesis, conjugation and transport, as well as lipid metabolism through actions in the liver and intestine. The first publication about fexaramine in 2003 showed it has 100-fold greater affinity for FXR than natural compounds and described the genomic targets and binding site on FXR.; When administered orally to mice, fexaramine produced selective actions through FXR receptors in the intestines. Consistent with the effects of other FXR agonist drugs, in a study in mice, oral fexaramine stimulated intestinal fibroblast growth factor 15 (FGF15) production and resulted in metabolic improvements.

The tissue response (y-axis) to an agonist, in log concentration (x-axis), in the presence of different antagonist concentrations. The EC50 of the agonist is represented by the x co-ordinate that corresponds with the half-maximum of the leftmost curve. This is denoted by [A] Half maximal effective concentration (EC50) refers to the concentration of a drug, antibody or toxicant which induces a response halfway between the baseline and maximum after a specified exposure time.Introducing dose response curves , Graphpad Software More simply, EC50 can be defined as the concentration required to obtain a 50% [...] effect EC50 estimation of antioxidant activity in DPPH assay using several statistical programs and may be also written as [A]50.

Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor. Ramelteon demonstrates full agonist activity in vitro in cells expressing human MT1 or MT2 receptors, and high selectivity for human MT1 and MT2 receptors compared to the MT3 receptor. The activity of ramelteon at the MT1 and MT2 receptors is believed to contribute to its sleep-promoting properties, as these receptors, acted upon by endogenous melatonin, are thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle. Ramelteon has no appreciable affinity for the GABA receptor complex or for receptors that bind neuropeptides, cytokines, serotonin, dopamine, noradrenaline, acetylcholine, and opioids.

27-Hydroxycholesterol (27-HC) is an endogenous oxysterol with multiple biological functions, including activity as a selective estrogen receptor modulator (SERM) (a mixed, tissue-specific agonist-antagonist of the estrogen receptor (ER)) and as an agonist of the liver X receptor (LXR). It is a metabolite of cholesterol that is produced by the enzyme CYP27A1. A link between high cholesterol and breast cancer has been identified, and it has been proposed that this is due to 27-HC production by CYP27A1. Because of its estrogenic action, 27-HC stimulates the growth of ER-positive breast cancer cells, and has been implicated in limiting the effectiveness of aromatase inhibitors in the treatment of breast cancer.

JWH-018 (1-pentyl-3-(1-naphthoyl)indole) or AM-678 is an analgesic chemical from the naphthoylindole family that acts as a full agonist at both the CB1 and CB2 cannabinoid receptors, with some selectivity for CB2. It produces effects in animals similar to those of tetrahydrocannabinol (THC), a cannabinoid naturally present in cannabis, leading to its use in synthetic cannabis products that in some countries are sold legally as "incense blends". As a full agonist at both the CB1 and CB2 cannabinoid receptors, this chemical compound is classified as an analgesic medication. The analgesic effects of cannabinoid ligands, mediated by CB1 receptors are well established in treatment of neuropathic pain, as well as cancer pain and arthritis.

Tonazocine (WIN-42,156) is an opioid analgesic of the benzomorphan family which made it to phase II clinical trials for the treatment of postoperative pain, but development was apparently ceased and ultimately it was never marketed. Tonazocine is a partial agonist at both the mu-opioid and delta- opioid receptors, but acting more like an antagonist at the former and more like an agonist at the latter. It lacks most of the side effects of other opioids such as adverse effects on the cardiovascular system and respiratory depression, but it can cause sedation (although to a lesser degree of typical opioids), and in some patients it may induce hallucinations (probably via binding to and activating the κ-opioid receptor).

125–169 Quite rapidly, between 20 and 90 minutes after ingestion, a substantial fraction of ibotenic acid is excreted unmetabolised in the urine of the consumer. Almost no muscimol is excreted when pure ibotenic acid is eaten, but muscimol is detectable in the urine after eating A. muscaria, which contains both ibotenic acid and muscimol. Ibotenic acid and muscimol are structurally related to each other and to two major neurotransmitters of the central nervous system: glutamic acid and GABA respectively. Ibotenic acid and muscimol act like these neurotransmitters, muscimol being a potent GABAA agonist, while ibotenic acid is an agonist of NMDA glutamate receptors and certain metabotropic glutamate receptors which are involved in the control of neuronal activity.

SM-130686 is a small-molecule drug which acts as a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue, with around half the potency of the endogenous agonist ghrelin as a stimulator of growth hormone release. It produces dose-dependent increases in muscle mass and decrease in body fat, and is under investigation for the treatment of growth hormone deficiency and other medical conditions. Concerns about its potential use as a performance-enhancing drug for athletes have led to the development of urine tests for SM-130686 and other GHSR agonists, even though no drugs from this class have yet progressed to clinical use.

The authors suggested that tianeptine may be acting as a biased agonist of the MOR and that this may be responsible for its atypical profile as a MOR agonist. However, there are reports that suggest that withdrawal effects resembling those of other typical opioid drugs (including but not limited to depression, insomnia, and cold/flu- like symptoms) do manifest following prolonged usage of dose usage far beyond the medical range. In addition to its therapeutic effects, activation of the MOR is likely to also be responsible for the abuse potential of tianeptine at high doses that are well above the normal therapeutic range. When co- administered with morphine, tianeptine prevents morphine-induced respiratory depression without impairing analgesia.

Ethylketazocine (WIN-35,197-2), is an opioid drug of the benzomorphan family which has been used extensively in scientific research in the last few decades as a tool to aid in the study of the κ-opioid receptor. However, due to its relatively poor selectivity for the κ-opioid receptor over the μ- and δ-opioid receptors (of which it has approximately 80% and 20% of the affinity for, respectively, in comparison), as well as its relatively poor intrinsic activity at all sites (i.e., acts as a partial agonist with mixed agonist and antagonist properties), it has been mostly replaced in recent times by newer and more potent and selective compounds like U-50,488 and ICI-199,441.

Cetrorelix is marketed by Merck Serono for use in in-vitro fertilization in all countries except Japan, where it is marketed by Shionogi and Nippon Kayaku.Aeternia Zentaris product page Aeterna Zentaris receives royalties on these sales and retains rights to develop cetrorelix for other indications. In IVF use it is injected daily after follicle stimulation has been initiated and evidence of follicle maturation is approaching; given daily it prevents an endogenous LH surge that would trigger an untimely ovulation prior to the hCG administration by the treating physician. As an alternative to the GnRH antagonist, also a GnRH agonist could be given, but agonist have to be started earlier to overcome the agonistic effect.

Serotonin modulator and stimulators (SMSs), sometimes referred to more simply as "serotonin modulators", are a type of drug with a multimodal action specific to the serotonin neurotransmitter system. To be precise, SMSs simultaneously modulate one or more serotonin receptors and inhibit the reuptake of serotonin. The term was coined in reference to the mechanism of action of the serotonergic antidepressant vortioxetine, which acts as a serotonin reuptake inhibitor (SRI), partial agonist of the 5-HT1A receptor, and antagonist of the 5-HT3 and 5-HT7 receptors. However, it can also technically be applied to vilazodone, which is an antidepressant as well and acts as an SRI and 5-HT1A receptor partial agonist.

A serotonin modulator and stimulator (SMS), sometimes referred to more simply as a serotonin modulator, is a type of drug with a multimodal action specific to the serotonin neurotransmitter system. To be precise, SMSs simultaneously modulate one or more serotonin receptors and inhibit the reuptake of serotonin. The term was created to describe the mechanism of action of the serotonergic antidepressant vortioxetine, which acts as a serotonin reuptake inhibitor (SRI), agonist of the 5-HT1A receptor, and antagonist of the 5-HT3 and 5-HT7 receptors. However, it can also technically be applied to vilazodone, which is an antidepressant as well and acts as an SRI and 5-HT1A receptor partial agonist.

Pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A receptors with high binding affinity (Ki 0.087 nM) and at serotonin 5-HT2C receptors with lower binding affinity (Ki 0.44 nM). Pimavanserin shows low binding to σ1 receptors (Ki 120 nM) and has no appreciable affinity (Ki >300 nM) to serotonin 5-HT2B, dopamine (including D2), muscarinic acetylcholine, histamine, or adrenergic receptors, or to calcium channels. Pimavanserin has a unique mechanism of action relative to other antipsychotics, behaving as a selective inverse agonist of the serotonin 5-HT2A receptor, with 40-fold selectivity for this site over the 5-HT2C receptor and no significant affinity or activity at the 5-HT2B receptor or dopamine receptors.

IBNtxA, or 3-iodobenzoyl naltrexamine, is an atypical opioid analgesic drug derived from naltrexone. In animal studies it produces potent analgesic effects that are blocked by levallorphan and so appear to be μ-opioid mediated, but it fails to produce constipation or respiratory depression, and is neither rewarding or aversive in conditioned place preference protocols. These unusual properties are thought to result from agonist action at a splice variant or heterodimer of the μ-opioid receptor, rather than at the classical full length form targeted by conventional opioid drugs.Keck TM, Uddin MM, Babenko E, Wu C, Moura-Letts G. Abuse Liability and Anti-Addiction Potential of the Atypical Mu Opioid Receptor Agonist IBNtxA.

Buserelin is a GnRH agonist, or an agonist of the GnRH receptor. It is a superagonist of the GnRH receptor with potency for induction of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion of about 20 to 170 times that of GnRH itself. By activating the GnRH receptor in the pituitary gland, buserelin induces the secretion of LH and FSH from the gonadotrophs of the anterior pituitary, which travel to the gonads through the bloodstream and activate gonadal sex hormone production as well as stimulate spermatogenesis in men and induce ovulation in women. With chronic administration of buserelin however, the GnRH receptor becomes desensitized and completely stops responding both to buserelin and to endogenous GnRH.

In 2010, nine people died due to the combination of O-desmethyltramadol, a μ-opioid agonist and analgesic drug, and Kratom, an Asiatic medicinal plant containing mitragynine, another μ-opioid agonist, in a synthetic cannabinoid product called "Krypton." In 2013, AH-7921 was detected in smoking blends in Japan. In 2018, there was an outbreak of synthetic cannabinoids contaminated with anticoagulants, mainly brodifacoum, in at least 11 states in the US that caused coagulopathy (prolonged or excessive bleeding) and resulted in the treatment of over 300 people and at least eight deaths. One of the most common non-cannabinoid ingredients in these products is oleamide, a fatty acid derivative that acts similarly to a cannabinoid and has hypnotic properties.

Moonbathers is the fifth studio album by the Dutch symphonic metal band Delain. It was released on 26 August 2016 worldwide. It features one guest appearance from Alissa White-Gluz (Arch Enemy, ex-The Agonist). Just like We Are the Others, this album does not feature Marco Hietala (Nightwish, Tarot).

The first published synthesis and pharmacological evaluation of APICA revealed that it acts as a full agonist at CB1 (EC50 = 34 nM) and CB2 receptors (EC50 = 29 nM). Furthermore, APICA possesses cannabis-like effects in rats, and appears to be less potent than JWH-018 but more potent than THC.

A cell stimulated with poly I: C (a synthetic TLR3 receptor agonist) with low doses of poly I: C increase iPSC production but higher levels decrease IPSC. It means if the innate immune response is inhibited or the response is disproportionately large, the cell will not be reprogrammed („Goldilocks zone“).

Detomidine is an imidazole derivative and α2-adrenergic agonist, used as a large animal sedative, primarily used in horses. It is usually available as the salt detomidine hydrochloride. It is a prescription medication available to veterinarians sold under the trade name Dormosedan. Currently, detomidine is only licensed for use in horses.

Remifentanil, being a μ-receptor agonist, functions like other μ-receptor agonists, such as morphine and codeine, and can cause euphoria and has the potential for abuse.Ternes, J. W., & O'Brien, C. P. (1990). The opioids: Abuse liability and treatments for dependence. Advances in alcohol & substance abuse, 9(1-2), 27-45.

Medetomidine is a synthetic drug used as both a surgical anesthetic and analgesic. It is often used as the hydrochloride salt, medetomidine hydrochloride, a crystalline white solid. It is an α2 adrenergic agonist that can be administered as an intravenous drug solution with sterile water. It was developed by Orion Pharma.

MDMA has been reported to be both a potent direct agonist and have an indirect effect by increasing plasma serotonin levels.Zolkowska, D., Rothman, R. B., & Baumann, M. H. (2006). Amphetamine analogs increase plasma serotonin: implications for cardiac and pulmonary disease. Journal of Pharmacology and Experimental Therapeutics, 318(2), 604-610.

NBUMP is a highly selective 5-HT1A receptor partial agonist (Ki = 0.1 nM; IA = 40%) with an arylpiperazine structure. It is one of the highest affinity ligands for the 5-HT1A receptor known. It displays 460- and 260-fold selectivity for 5-HT1A over the α1-adrenergic and D2 receptors, respectively.

Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Formerly, it was also used to prolong the action of local anesthetics. It is the ketone form of epinephrine (adrenaline). Contrary to epinephrine, adrenalone mainly acts on alpha-1 adrenergic receptors, but has little affinity for beta receptors.

Anionic lipids compete for binding sites within ion channel. Similar to neurotransmitters, competition of an antagonist reverses the effect of an agonist. In most cases, the PA has the opposite effect of PIP2. Hence when PA binds to a channel that is activated by PIP2, PA inhibits the effect of PIP2.

Tibolone is a Schedule IV controlled substance in Canada under the 1996 Controlled Drugs and Substances Act. It is classified as an anabolic steroid under this act, due to its relatively high activity as an agonist, and is the only norethisterone (17α-ethynyl-19-nortestosterone) derivative that is classified as such.

Most grid cells from layer III do not precess, but their spike activity is largely confined to half of the theta cycle. The grid cell phase precession is not derived from the hippocampus, because it continues to appear in animals whose hippocampus has been inactivated by an agonist of GABA.

Terbequinil (SR-25776) is a stimulant and nootropic drug which acts as a partial inverse agonist at benzodiazepine sites on the GABAA receptor. In human trials it was found to partially reverse the sedative and amnestic effects of the hypnotic drug triazolam with only slight effects when administered by itself.

It acts as an NMDA receptor agonist. Quinolinic acid has a potent neurotoxic effect. Studies have demonstrated that quinolinic acid may be involved in many psychiatric disorders, neurodegenerative processes in the brain, as well as other disorders. Within the brain, quinolinic acid is only produced by activated microglia and macrophages.

Harmaline, a Beta-carboline Beta-carbolines are "reversible" MAO-A inhibitors. They are found in some plants used to make Ayahuasca. In high doses the harmala alkaloids are somewhat hallucinogenic on their own. β-carboline is a benzodiazepine receptor inverse agonist and can therefore have convulsive, anxiogenic and memory enhancing effects.

Sulfur analogs are known with a benzothienyl replacement as well as 4-SH-DMT.A Hofmann, F Troxler, Swiss 421,960 (1967); CA 68:95680n 1-Methylpsilocin is a functionally 5-HT2C receptor preferring agonist. 4-Fluoro-N,N-dimethyltryptamine is known. O-Acetylpsilocin (4-AcO-DMT) is an acetylated analog of psilocin.

5F-PB-22 (5F-QUPIC or quinolin-8-yl 1-pentyfluoro-1H-indole-3-8-carboxylate) is a designer drug which acts as a cannabinoid agonist. The structure of 5F-PB-22 appears to have been designed with an understanding of structure–activity relationships within the indole class of cannabinoids.

These papers also show that the key modulator for excitation- inhibition balance in the brain is mainly dependent on the levels of glutamate and GABA. In addition to glutamate, Best1 can also release d-serine, which can act as a co-agonist of NMDA receptors to participate in synaptic plasticity.

Certain members of the 15-hydroxyeicosatetraenoic acid family of arachidonic acid metabolites, including 15(S)-HETE, 15(R)-HETE, and 15-HpETE activate to varying degrees PPAR alpha, beta/delta, and gamma.Mol. Pharmacol. 77-171-184, 2010 PPARγ activation by agonist RS5444 may inhibit anaplastic thyroid cancer growth. SeeCurr. Mol. Med.

Serious side effects may include low blood pressure, liver problems, psychosis, and QT prolongation. It is unclear if use in pregnancy and breastfeeding is safe. It is an α2-adrenergic agonist and how it works is not entirely clear. Tizanidine was approved for medical use in the United States in 1996.

This allows beta carboline to act as an inverse agonist and reduce the current below basal levels. Mutations in receptors that result in increased constitutive activity underlie some inherited diseases, such as precocious puberty (due to mutations in luteinizing hormone receptors) and hyperthyroidism (due to mutations in thyroid-stimulating hormone receptors).

BIM-018 is a synthetic cannabinoid that is the benzimidazole analog of JWH-018. It is presumed to be a potent agonist of the CB2 receptor and has been sold online as a designer drug. Related benzimidazole derivatives have been reported to be highly selective agonists for the CB2 receptor.

Estradiol, the active form of PEP. PEP is an estradiol ester in the form of a polymer and is an extremely long-lasting prodrug of estradiol. As such, it is an estrogen, or an agonist of the estrogen receptors. PEP has antigonadotropic and functional antiandrogenic effects due to its estrogenic activity.

Farglitazar is a peroxisome proliferator-activated receptor agonist which was formerly under development by GlaxoSmithKline, but has never been marketed. It progressed to phase II clinical trials for the treatment of hepatic fibrosis, but failed to show efficacy. After reaching phase III for type 2 diabetes, further development was discontinued.

Conversely, rats do not express a splice variant homologous to the h5-HT7(d), as the rat 5-HT7 gene lacks the exon necessary to encode this isoform. Drug binding affinities are similar across the three human splice variants; however, inverse agonist efficacies appear to differ between the splice variants.

Fentanyl is a synthetic opioid structurally similar arylpiperidines. It is a strong μ-receptor agonist that is 80–100 times more potent to morphine, and has a fast onset with a shorter duration of action than morphine. It is metabolized in the liver by CYP3A4 enzymes to norfentanyl, an inactive drug.

Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific literature by Sumitomo Chemical as "β-adrenergic blocking, antiarrhythmic compound S-596".

E1R enhances cognition and has efficacy against cholinergic dysfunction in mice without affecting locomotor activity. Pretreatment with E1R enhanced the σ1R agonist PRE-084's stimulating effect and facilitated passive avoidance retention. It alleviated scopolamine-induced cognitive impairment. The cognition enhancing activity of E1R is higher than that of (R)-phenylpiracetam.

2,5-dimethoxy-4-bromophenylpiperazine (2C-B-PP) is a drug of the phenylpiperazine class. It acts as an agonist at serotonin receptors, and in studies on rats substituted for the psychedelic amphetamine derivative DOM with around 1/10th the potency but similar rates of stimulus-appropriate responding at the highest dose.

MMDA has been shown to act as a non-neurotoxic serotonin releasing agent with no effects on dopamine release and probably norepinephrine release as well, and as a 5-HT2A receptor agonist. The latter property is responsible for its psychedelic effects, whereas the former mediates its mood-lifting and empathogenic effects.

The compound is therefore expected to be a drug for the treatment of auto-immune diseases such as multiple sclerosis, which is regarded as an intractable disease. Ozanimod is an agonist of the S1P1 and S1P5 receptors. and has been studied for various forms of multiple sclerosis.New Frontiers in S1P Modulators.

Ipratropium bromide/salbutamol, sold under the brand name Combivent among others, is a combination medication used to treat chronic obstructive pulmonary disease (COPD). It contains ipratropium (an anticholinergic) and salbutamol (albuterol, a β2-adrenergic agonist). It is taken by inhalation. Common side effects include sore throat, muscle cramps, and nausea.

It is an estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. Methylestradiol is or has been marketed in Brazil, Venezuela, and Indonesia. In addition to its use as a medication, methylestradiol has been studied for use as a radiopharmaceutical for the estrogen receptor.

3,8-Dihydrodiligustilide is a nonsteroidal phytoprogestogen that is found in Ligusticum chuanxiong. It is a potent agonist of the progesterone receptor (EC50 = 90 nM). Another compound in the plant, riligustilide, is also a phytoprogestogen, but is almost 1,000-fold less potent and is very weak in comparison (EC50 ≈ 81 μM).

Gemazocine (R-15,497), also known as cyclogemine, is a non-selective opioid antagonist of the benzomorphan class. It may have partial agonist properties at some of the opioid receptors, such as at the kappa receptor (as it induces dysphoric effects in humans), but seems to be generally antagonistic in its actions.