A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action of serotonin and serotonergic drugs 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, but are not limited to:

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, but are not limited to:

Other 5-HT3 antagonists have been considered for use in the treatment of irritable bowel syndrome:

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

Non-selective 5-HT antagonists

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.

They include, but are not limited to:

Antihistamines with antiserotonergic activity


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). Pittler MH (ed.). "Feverfew for preventing migraine". Cochrane Database of Systematic Reviews (1): CD002286. doi:10.1002/14651858.CD002286.pub2. PMID 14973986.
  3. ^ Mittra, S; Datta, A; Singh, SK; Singh, A (December 2000). "5-Hydroxytryptamine-inhibiting property of Feverfew: role of parthenolide content". Acta Pharmacologica Sinica. 21 (12): 1106–14. PMID 11603284.
  4. ^ Chairungsrilerd, Nattaya; Furukawa, K.-I.; Ohta, Tomihisa; Nozoe, Shigeo; Ohizumi, Yasushi (12 December 1997). "γ-Mangostin, a novel type of 5-hydroxytryptamine 2A receptor antagonist". Naunyn-Schmiedeberg's Archives of Pharmacology. 357 (1): 25–31. doi:10.1007/pl00005134. PMID 9459569. S2CID 24972810.