Serotonin receptor antagonist

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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.[citation needed]
  • 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:

  • Dolasetron
  • Granisetron
  • Ondansetron
  • Palonosetron
  • Tropisetron

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

  • Alosetron
  • Cilansetron

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.[citation needed] 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[]

  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.

External links[]


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