Supriya Ghosh (Editor)

Serotonin antagonist

Updated on
Edit
Like
Comment
Share on FacebookTweet on TwitterShare on LinkedInShare on Reddit

Inhibitory effect of serotonin antagonist on leukocyte endothelial interactions in vivo and in vitro


A serotonin antagonist is a drug used to inhibit the action at serotonin (5-HT) receptors.

Contents

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.
  • 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
  • Non-selective 5-HT antagonists

    Please note, that although some non-selective serotonin antagonists may have an particular affinity for a specific 5-HT receptor (and thus may be listed above e.g. methysergide), they still may also possess a generalised non-selective action.

  • Methysergide
  • Chlorpromazine
  • Cyproheptadine
  • Pizotifen
  • Oxetorone
  • Spiperone
  • Ritanserin
  • Parachlorophenylalanine
  • Metergoline
  • Propranolol
  • Mianserin
  • Serotonin antagonists acting as antihistamines for allergic conditions

  • Carbinoxamine
  • Cyproheptadine
  • Methdilazine
  • Promethazine
  • Pizotifen is a 5-HT2C antagonist, H1 blocker and anticholinergic useful in migraine prophylaxis. Also used in the treatment of migrane.
  • oxetorone Also used in the treatment of migrane.
  • Oxatomide
  • Others

  • Feverfew Is a herb traditionally used for migraines.
  • Fenclonine An inhibitor of serotonin synthesis that has been used in the treatment of carcinoid syndrome.
  • Reserpine Depletes serotonin stores in the brain, heart, and many other organs and has been used in hypertension and psychosis
  • References

    Serotonin antagonist Wikipedia


    Similar Topics