5-HT3 Receptor Antagonists in Neurologic and Neuropsychiatric Disorders: The Iceberg Still Lies beneath the Surface

Pharmacol Rev. 2019 Jul;71(3):383-412. doi: 10.1124/pr.118.015487.

Abstract

5-HT3 receptor antagonists, first introduced to the market in the mid-1980s, are proven efficient agents to counteract chemotherapy-induced emesis. Nonetheless, recent investigations have shed light on unappreciated dimensions of this class of compounds in conditions with an immunoinflammatory component as well as in neurologic and psychiatric disorders. The promising findings from multiple studies have unveiled several beneficial effects of these compounds in multiple sclerosis, stroke, Alzheimer disease, and Parkinson disease. Reports continue to uncover important roles for 5-HT3 receptors in the physiopathology of neuropsychiatric disorders, including depression, anxiety, drug abuse, and schizophrenia. This review addresses the potential of 5-HT3 receptor antagonists in neurology- and neuropsychiatry-related disorders. The broad therapeutic window and high compliance observed with these agents position them as suitable prototypes for the development of novel pharmacotherapeutics with higher efficacy and fewer adverse effects.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Mental Disorders / drug therapy*
  • Mental Disorders / metabolism
  • Nervous System Diseases / drug therapy*
  • Nervous System Diseases / metabolism
  • Receptors, Serotonin, 5-HT3 / metabolism
  • Serotonin 5-HT3 Receptor Antagonists / pharmacology*
  • Serotonin 5-HT3 Receptor Antagonists / therapeutic use*

Substances

  • Receptors, Serotonin, 5-HT3
  • Serotonin 5-HT3 Receptor Antagonists

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