Serotonin receptor antagonist

A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action 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:

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 antidepressant Clozapine antipsychotic. Blocks 5-HT2A, 5-HT2C and D4 receptors. Nefazodone acts primarily as a potent 5-HT2A antagonist. 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:

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 Please note, that 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 generalized non-selective action.

Chlorpromazine Cyproheptadine Metergoline Methysergide Mianserin Mirtazapine Oxetorone Pizotifen Propranolol Ritanserin Spiperone 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 migraine. Oxatomide Oxetorone Also used in the treatment of migraine. 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. Reserpine Depletes serotonin stores in the brain, heart, and many other organs and has been used in hypertension and psychosis.

Studies have shown that retrieval of long-term memory can cause memory reconsolidation, and impaired reconsolidation leads to amnesia development. However, the mechanisms of amnesia induction due to impaired memory reconsolidation remains poorly described. Using experiments involving grape snails trained to conditioned food aversion, we studied the role of translation and transcription processes and the role of serotonin receptors in the mechanisms of amnesia induction. We found that administration of a serotonin receptor antagonist or a protein synthesis inhibitor before the administration of a reminder using a conditioned food stimulus induced amnesia development, whereas injections of mRNA synthesis inhibitor did not affect memory safety. Moreover, combined injections of an antagonist of serotonin receptor and inhibitors of protein or mRNA synthesis before reminder administration completely prevented amnesia development. In addition, inhibitors of protein or mRNA synthesis prevented amnesia development 3 h but not 9 h after the administration of a serotonin receptor antagonist/reminder. We hypothesize that the mechanisms of amnesia induction caused by impaired memory reconsolidation depend on protein and mRNA syntheses within a certain time window, similar to the mechanisms of induction of other long-term plastic brain rearrangements ¹⁾.