Impact of 5-HT₃ receptor antagonists on peripheral and central diseases

Drug Discov Today. 2012 Jul;17(13-14):741-7. doi: 10.1016/j.drudis.2012.02.009. Epub 2012 Feb 25.


In this article we discuss the novel pharmacological aspects of 5-HT(3) receptor antagonists. Commonly used to counteract chemotherapy-induced emesis, these agents now appear to be reaching out for newer indications. Studies have reported neuroprotective and anti-inflammatory properties in vitro and in vivo. 5-HT(3) receptor antagonists can modulate the immune-inflammatory axis through blockade of 5-HT(3) receptors present on immune cells. We review evidence addressing the effects of these drugs on peripheral inflammatory diseases, including asthma, rheumatoid diseases, inflammatory bowel disease and sepsis in addition to diabetes and CNS disorders, including Alzheimer's disease (AD), seizure and stroke.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Central Nervous System Diseases / drug therapy*
  • Central Nervous System Diseases / immunology
  • Central Nervous System Diseases / metabolism
  • Clinical Trials as Topic
  • Drug Discovery*
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / immunology
  • Inflammation / metabolism
  • Molecular Structure
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / pharmacology
  • Neuroprotective Agents / therapeutic use*
  • Receptors, Serotonin, 5-HT3 / metabolism
  • Serotonin 5-HT3 Receptor Antagonists / chemistry
  • Serotonin 5-HT3 Receptor Antagonists / pharmacology
  • Serotonin 5-HT3 Receptor Antagonists / therapeutic use*


  • Anti-Inflammatory Agents
  • Neuroprotective Agents
  • Receptors, Serotonin, 5-HT3
  • Serotonin 5-HT3 Receptor Antagonists