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.