Betahistine: what's new on the agenda?

Expert Opin Investig Drugs. 2008 May;17(5):795-804. doi: 10.1517/13543784.17.5.795.


Background: Betahistine is an orally administered, centrally acting histamine H(1) receptor agonist with partial H(3) antagonistic activity and no H(2)-binding effects. In the past betahistine was clinically studied mainly as a vasodilator for conditions such as cluster headaches, vascular dementia and Meniere's disease, for which it is still used. In recent years, histamine was found to be a key neurotransmitter in the regulation of feeding behavior.

Objective: To provide a review of the developmental history and current research interests of betahistine.

Methods: All reports of betahistine use in animals and humans were retrieved and reviewed.

Results/conclusion: The unique pharmacologic properties of betahistine point to its potential future use as an antiobesity agent.

Publication types

  • Review

MeSH terms

  • Animals
  • Betahistine* / chemistry
  • Betahistine* / pharmacology
  • Betahistine* / therapeutic use
  • Clinical Trials as Topic
  • Cluster Headache / drug therapy
  • Cluster Headache / metabolism
  • Drug Evaluation
  • Histamine Agonists* / chemistry
  • Histamine Agonists* / pharmacology
  • Histamine Agonists* / therapeutic use
  • Humans
  • Meniere Disease / drug therapy
  • Meniere Disease / metabolism
  • Molecular Structure
  • Obesity / drug therapy
  • Obesity / metabolism
  • Receptors, Histamine H1 / metabolism


  • Histamine Agonists
  • Receptors, Histamine H1
  • Betahistine