A serotonin receptor agonist is a compound that activates serotonin receptors, mimicking the effect of the neurotransmitter serotonin

Serotonin

Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...

. There are various serotonin receptors and ligands.

5-HT_1A receptor

Azapirones such as buspirone

Buspirone

Buspirone is an anxiolytic psychoactive drug of the azapirone chemical class, and is primarily used to treat generalized anxiety disorder Bristol-Myers Squibb gained FDA approval of buspirone in 1986 for treatment of GAD...

, gepirone

Gepirone

Gepirone is a psychoactive drug and research chemical of the piperazine and azapirone chemical classes. It is currently under clinical development in an extended release form as an anxiolytic and antidepressant agent...

, and tandospirone

Tandospirone

Tandospirone , also known as metanopirone, is an anxiolytic and antidepressant used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma...

 are 5-HT_1A agonists marketed primarily as anxiolytic

Anxiolytic

An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...

s, but also recently as antidepressant

Antidepressant

An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...

s.

5-HT_1B receptor

Triptan

Triptan

Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. They were first introduced in the 1990s...

s such as sumatriptan

Sumatriptan

Sumatriptan is a triptan sulfa drug containing a sulfonamide group. It is used for the treatment of migraine headaches. Sumatriptan is produced and marketed by various drug manufacturers with many different trade names such as Sumatriptan, Imitrex, Imigran, Imigran recovery.-Approval and...

, rizatriptan

Rizatriptan

Rizatriptan is a 5-HT1 agonist triptan drug developed by Merck & Co. for the treatment of migraine headaches. It is available in strengths of 5 and 10 mg as tablets and orally disintegrating tablets ....

, and naratriptan

Naratriptan

Naratriptan is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches. Naratriptan is available in 2.5 mg tablets. It is a selective 5-HT1 receptor subtype agonist...

, are 5-HT_1B receptor agonists that are used to abort migraine

Migraine

Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...

 and cluster headache

Cluster headache

Cluster headache, nicknamed "suicide headache", is a neurological disease that involves, as its most prominent feature, an immense degree of pain in the head. Cluster headaches occur periodically: spontaneous remissions interrupt active periods of pain. The cause of the disease is currently unknown...

 attacks.

5-HT_1D receptor

In addition to being 5-HT_1B agonists, triptan

Triptan

Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. They were first introduced in the 1990s...

s are also agonists at the 5-HT_1D receptor, which contributes to their antimigraine effect.

5-HT_1F receptor

LY-334,370 was a selective 5-HT_1F agonist that was being developed by Eli Lilly and Company

Eli Lilly and Company

Eli Lilly and Company is a global pharmaceutical company. Eli Lilly's global headquarters is located in Indianapolis, Indiana, in the United States...

 for the treatment of migraine and cluster headaches. Development was halted however due to toxicity detected in animal test subjects. Lasmiditan

Lasmiditan

Lasmiditan is an investigational drug for the treatment of acute migraine. It was discovered by Eli Lilly and Company and is being developed by CoLucid Pharmaceuticals...

 has successfully completed Phase II clinical trials in early 2010.

5-HT_2A receptor

Psychedelic drug

Psychedelic drug

A psychedelic substance is a psychoactive drug whose primary action is to alter cognition and perception. Psychedelics are part of a wider class of psychoactive drugs known as hallucinogens, a class that also includes related substances such as dissociatives and deliriants...

s such as LSD

LSD

Lysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide and colloquially as acid, is a semisynthetic psychedelic drug of the ergoline family, well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synaesthesia, an...

, mescaline

Mescaline

Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally occurring psychedelic alkaloid of the phenethylamine class used mainly as an entheogen....

, psilocin

Psilocin

Psilocin , an aromatic compound, sometimes also spelled psilocine, psilocyn, or psilotsin, is a psychedelic mushroom alkaloid. It is found in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin...

, DMT

Dimethyltryptamine

N,N-Dimethyltryptamine is a naturally occurring psychedelic compound of the tryptamine family. DMT is found in several plants, and also in trace amounts in humans and other mammals, where it is originally derived from the essential amino acid tryptophan, and ultimately produced by the enzyme INMT...

, and 2C-B

2C-B

2C-B or 4-bromo-2,5-dimethoxyphenethylamine is a psychedelic drug of the 2C family. It was first synthesized by Alexander Shulgin in 1974. In Shulgin's book PiHKAL, the dosage range is listed as 16–24 mg. 2C-B is sold as a white powder sometimes pressed in tablets or gel caps and is referred...

 act as 5-HT_2A agonists. Their action at this receptor is responsible for their hallucinogenic effects.

It is now known that many of these drugs act as agonists at many other 5HT receptors in addition to the 5-HT2A including the 5-HT2C and others.

5-HT_2C receptor

Lorcaserin

Lorcaserin

Lorcaserin is a weight-loss drug developed by Arena Pharmaceuticals. It has serotonergic properties and acts as an anorectic. On 22 December 2009 a New Drug Application was submitted to the Food and Drug Administration in the United States and lorcaserin is pending approval...

 is a thermogenic and anorectic

Anorectic

An anorectic or anorexic , also known as anorexigenic or appetite suppressant, is a dietary supplement and/or drug which reduces appetite, food consumption, and as a result, causes weight loss to occur.-List of anorectics:Numerous pharmaceutical compounds are marketed as appetite suppressants.The...

 weight-loss drug which acts as a selective 5-HT_2C agonist.

5-HT₄ receptor

Cisapride

Cisapride

Cisapride is a gastroprokinetic agent, a drug which increases motility in the upper gastrointestinal tract. It acts directly as a serotonin 5-HT4 receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous...

 is a 5-HT₄ partiel receptor agonist that has been used to treat disorders of gastrointestinal motility.
Prucalopride is a highly selective 5-HT₄ receptor agonist that can be used to treat certain disorders of gastrointestinal motility

5-HT₇ receptor

AS-19 (drug)

AS-19 (drug)

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....

is a 5-HT₇ receptor agonist that has been used only in research.

External links

• IUPHAR GPCR Database - 5-HT receptor family