Serotonin receptor agonist

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A serotonin receptor agonist is a compound that activates serotonin receptors, in a manner similar to serotonin.

Non-selective agonists: Psilocin and DMT are serotonin analogs found in certain plants or mushrooms. These compounds act on a variety of serotonin receptor types.

5-HT1A agonists[edit]

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

5-HT1B agonists[edit]

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

5-HT1D agonists[edit]

In addition to being 5-HT1B agonists, triptans are also agonists at the 5-HT1D receptor, which contributes to their antimigraine effect caused by vasoconstriction of blood vessels in the brain.

5-HT1F agonists[edit]

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 is slow however due to toxicity detected in animal test subjects.

5-HT2A agonists[edit]

Psychedelic drugs like LSD, mescaline, and 2C-B, act as 5-HT2A agonists. Their action at this receptor is responsible for their "psychedelic" effects. Some of these drugs, act as agonists for other 5HT receptor subtypes. Not all 5-HT2A agonists are psychoactive.[1]

5-HT2B agonists[edit]

Drugs that act as agonists on this receptor are implicated in the progression of cardiac fibrosis.[2] Fenfluramine, Pergolide and Cabergoline have been withdrawn from some markets for this reason.[3] Some psychedelic drugs, including LSD and Psilocin, have been shown to activate this receptor directly.[4] MDMA has been reported to be both a potent direct agonist[5] and have an indirect effect by increasing plasma serotonin levels.[6]

5-HT2C agonists[edit]

Lorcaserin is a thermogenic and anorectic weight-loss drug which acts as a selective 5-HT2C agonist.

5-HT4 agonists[edit]

Cisapride and Tegaserod are 5-HT4 partial receptor agonist that were 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. Other 5-HT4 agonists have shown potential to be nootropic type drugs via promoting acetylcholine release.

5-HT7 agonists[edit]

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

See also[edit]


  1. ^ Aghajanian, M.D., G.K.; G.J. Marek, M.D., Ph.D. (1999). "Serotonin and Hallucinogens". Neuropharmacology 21 (2S): 16S. doi:10.1016/s0893-133x(98)00135-3. 
  2. ^ Hutcheson, J. D., Setola, V., Roth, B. L., & Merryman, W. D. (2011). Serotonin receptors and heart valve disease—it was meant 2B. Pharmacology & therapeutics, 132(2), 146-157.
  3. ^ Brea, J., Castro-Palomino, J., Yeste, S., Cubero, E., Párraga, A., Domínguez, E., & Loza, M. I. (2010). Emerging Opportunities and Concerns for Drug Discovery at Serotonin 5-HT2B Receptors. Current topics in medicinal chemistry, 10(5), 493-503.
  4. ^ Halberstadt, A. L., & Geyer, M. A. (2011). Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens. Neuropharmacology, 61(3), 364-381.
  5. ^ Hutcheson, J. D., Setola, V., Roth, B. L., & Merryman, W. D. (2011). Serotonin receptors and heart valve disease—it was meant 2B. Pharmacology & therapeutics, 132(2), 146-157.
  6. ^ 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.

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