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Serotonin receptor antagonist

Neurotransmission-modulating substance

Neurotransmission-modulating substance

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.

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
  • Nefazodone

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.

They include, but are not limited to:

  • Dolasetron
  • Granisetron
  • Ondansetron
  • Palonosetron
  • Tropisetron

Other 5-HT3 antagonists have been considered for use in 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:

  • Chlorpromazine
  • Cyproheptadine
  • Metergoline
  • Methysergide
  • Mianserin
  • Mirtazapine
  • Oxetorone
  • Pizotifen
  • Propranolol
  • Ritanserin
  • Spiperone

Antihistamines with antiserotonergic activity

  • Carbinoxamine
  • Cinnarizine
  • 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 Is a herb traditionally used for migraines (contains parthenolide).
  • 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

References

References

  1. (September 2000). "Oral serotonin type 3-receptor antagonists for prevention of chemotherapy-induced emesis". American Journal of Health-System Pharmacy.
  2. (2004). "Feverfew for preventing migraine". The Cochrane Database of Systematic Reviews.
  3. (December 2000). "5-Hydroxytryptamine-inhibiting property of Feverfew: role of parthenolide content". Acta Pharmacologica Sinica.
  4. (January 1998). "Gamma-mangostin, a novel type of 5-hydroxytryptamine 2A receptor antagonist". Naunyn-Schmiedeberg's Archives of Pharmacology.
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