Serotonin receptor antagonist
A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors.
Types
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:
- Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic.
- Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis.
- Quetiapine blocks 5-HT2A, 5-HT1A, dopamine receptors D1 and D2, histamine receptor H1, and A1 adrenoreceptors.
5-HT2A/2C antagonists
- Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C and Alpha 1 (A1) adrenoreceptors.
- Risperidone antipsychotic
- Trazodone
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 are used for 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
- Carbinoxamine
- Cyproheptadine
- Hydroxyzine
- Methdilazine
- Pizotifen
- Promethazine
- Pizotifen is a 5-HT2C antagonist, H1 blocker and anticholinergic useful in migraine prophylaxis. Also used in the treatment of migrane.
- Oxatomide
- Oxetorone Also used in the treatment of migrane.
- Ketotifen
Others
- 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 (contains parthenolide[3]).
- Reserpine Depletes serotonin stores in the brain, heart, and many other organs and has been used in hypertension and psychosis
- Gamma-mangostin from Garcinia mangostana[4]
See also
References
- 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.
- 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.
- 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.
- 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.
External links
- Serotonin+Antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82012702