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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:
- 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
- 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.[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
- Carbinoxamine
- Cinnarizine
- 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]
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