Histamine H(3) receptor (H(3)R) antagonists and inverse agonists in the treatment of sleep disorders

Curr Pharm Des. 2011;17(15):1426-9. doi: 10.2174/138161211796197133.

Abstract

After the discovery and characterization of the H(3)R and H(4)R receptors, they have become widely anticipated as potential therapeutic agents in the treatment of sleep disorders. In preliminary studies, histamine H(3) receptor (H(3)R) antagonists and inverse agonists have demonstrated promise in the treatment of sleep disorders associated with excessive daytime sleepiness. This review article summarizes the current research in this area and characteristics of H(3)R and H(3)R antagonists and inverse agonists in development.

Publication types

  • Review

MeSH terms

  • Animals
  • Disorders of Excessive Somnolence / drug therapy*
  • Disorders of Excessive Somnolence / metabolism
  • Drug Design
  • Drug Inverse Agonism
  • Histamine Agonists / pharmacology
  • Histamine Agonists / therapeutic use*
  • Histamine H3 Antagonists / pharmacology
  • Histamine H3 Antagonists / therapeutic use*
  • Humans
  • Receptors, Histamine H3 / drug effects
  • Receptors, Histamine H3 / metabolism
  • Sleep Wake Disorders / drug therapy
  • Sleep Wake Disorders / metabolism

Substances

  • Histamine Agonists
  • Histamine H3 Antagonists
  • Receptors, Histamine H3