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-HT
2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists).
They include, but are not limited to:
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Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic.
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Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis.
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Quetiapine blocks 5-HT2A, 5-HT1A, dopamine receptors D1 and D2, histamine receptor H1, and a1 adrenoreceptors.
5-HT2A/2C antagonists
5-HT3 antagonists
Another subclass consists of drugs selectively acting at the 5-HT
3 receptors, and thus are known as 5-HT
3 antagonists. They are efficacious in treating chemotherapy-induced emesis and postoperative nausea and vomiting.
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
Others
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Fenclonine ( para-chlorophenylalanine; PCPA) An inhibitor of serotonin synthesis that has been used in the treatment of carcinoid syndrome.
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Feverfew
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Reserpine Depletes serotonin stores in the brain, heart, and many other organs and has been used in hypertension and psychosis
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Gamma-mangostin from Garcinia mangostana
See also
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Serotonin receptor agonist
External links
