Serotonin receptor antagonist
A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action of serotonin and serotonergic drugs at serotonin receptors.
Types
5-HT2A antagonists
Antagonists of the 5-HT2A receptor are sometimes used as atypical antipsychotics.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 adrenoreceptors.
- Risperidone antipsychotic
- Trazodone
- Nefazodone
5-HT3 antagonists
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, 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 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
- Gamma-mangostin from Garcinia mangostana