Serotonin receptor agonist

A serotonin receptor agonist is a compound that activates serotonin receptors, mimicking the effect of the neurotransmitter serotonin. There are various serotonin receptors and ligands.

5-HT_1A receptor

Azapirones such as buspirone, gepirone, and tandospirone are 5-HT_1A agonists marketed primarily as anxiolytics, but also recently as antidepressants.

5-HT_1B receptor

Triptans such as sumatriptan, rizatriptan, and naratriptan, are 5-HT_1B receptor agonists that are used to abort migraine and cluster headache attacks.

5-HT_1D receptor

In addition to being 5-HT_1B agonists, triptans 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 for the treatment of migraine and cluster headaches. Development was halted however due to toxicity detected in animal test subjects. Lasmiditan has successfully completed Phase II clinical trials in early 2010.

5-HT_2A receptor

Psychedelic drugs such as LSD, mescaline, psilocin, DMT, and 2C-B 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 is a thermogenic and anorectic weight-loss drug which acts as a selective 5-HT_2C agonist.

5-HT₄ receptor

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

See also

• Serotonin antagonist
• Agonist

External links

• IUPHAR GPCR Database - 5-HT receptor family
• MeSH list of agents 82017366
• MeSH Serotonin+agonists