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Serotonin receptor antagonist

A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors.


5-HT2A antagonists

Antagonists of the 5-HT2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). They include:

5-HT2A/2C antagonists

5-HT3 antagonists

Another subclass consists of drugs selectively acting at the 5-HT3 receptors, and thus are known as 5-HT3 antagonists. They are efficacious in treating chemotherapy-induced emesis and postoperative nausea and vomiting.[1] They include:

Other 5-HT3 antagonists are used for the treatment of irritable bowel syndrome:

Also, the antidepressant mirtazapine acts as a 5-HT3 antagonist.

Non-selective 5-HT antagonists

Please note, that although some non-selective serotonin antagonists may have a particular affinity for a specific 5-HT receptor (and thus may be listed below e.g., methysergide), they still may also possess a generalised non-selective action.

Antihistamines with antiserotonergic activity


  • Fenclonine (para-chlorophenylalanine; PCPA) An inhibitor of serotonin synthesis that has been used in the treatment of carcinoid syndrome.
  • Feverfew[2] Is a herb traditionally used for migraines.
  • Reserpine Depletes serotonin stores in the brain, heart, and many other organs and has been used in hypertension and psychosis

See also


  1. ^ Lindley, C.; Blower, P. (2000). "Oral serotonin type 3-receptor antagonists for prevention of chemotherapy-induced emesis". American Journal of Health-System Pharmacy. 57 (18): 1685–1697. doi:10.1093/ajhp/57.18.1685. PMID 11006796.
  2. ^ Pittler MH, Ernst E (2004). "Feverfew for preventing migraine". Cochrane Database of Systematic Reviews (1): CD002286. doi:10.1002/14651858.CD002286.pub2. PMID 14973986.

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