Serotonin receptor antagonist
A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors.
- 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.
- Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C and Alpha 1 (A1) adrenoreceptors.
- Risperidone antipsychotic
- Trazodone antidepressant
- Clozapine antipsychotic. Blocks 5-HT2A, 5-HT2C and D4 receptors.
- Nefazodone acts primarily as a potent 5-HT2A antagonist.
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. 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
- Pizotifen is a 5-HT2C antagonist, H1 blocker and anticholinergic useful in migraine prophylaxis. Also used in the treatment of migrane.
- Oxetorone Also used in the treatment of migrane.
- Fenclonine (para-chlorophenylalanine; PCPA) An inhibitor of serotonin synthesis that has been used in the treatment of carcinoid syndrome.
- Feverfew 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
- 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). "Feverfew for preventing migraine". Cochrane Database of Systematic Reviews (1): CD002286. doi:10.1002/14651858.CD002286.pub2. PMID 14973986.
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- Serotonin+Antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82012702
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