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-HT1A receptor
Azapirones such as buspirone, gepirone, and tandospirone are 5-HT1A agonists marketed primarily as anxiolytics, but also recently as antidepressants.

5-HT1B receptor
Triptans such as sumatriptan, rizatriptan, and naratriptan, are 5-HT1B receptor agonists that are used to abort migraine and cluster headache attacks.

5-HT1D receptor
In addition to being 5-HT1B agonists, triptans are also agonists at the 5-HT1D receptor, which contributes to their antimigraine effect.

5-HT1F receptor
LY-334,370 was a selective 5-HT1F 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-HT2A receptor
Psychedelic drugs such as LSD, mescaline, psilocin, DMT, and 2C-B act as 5-HT2A 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-HT2C receptor
Lorcaserin is a thermogenic and anorectic weight-loss drug which acts as a selective 5-HT2C agonist.

5-HT4 receptor
Cisapride is a 5-HT4 receptor agonist that has been used to treat disorders of gastrointestinal motility.

5-HT7 receptor
AS-19 (drug) is a 5-HT7 receptor agonist that has been used only in research.