Selective orexin receptor antagonists

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4761-9. doi: 10.1016/j.bmcl.2013.06.057. Epub 2013 Jul 4.

Abstract

The orexin, or hypocretin, neuropeptides (orexin-A and orexin-B) are produced on neurons in the hypothalamus which project to key areas of the brain that control sleep-wake states, modulation of food intake, panic, anxiety, emotion, reward and addictive behaviors. These neuropeptides exert their effects on a pair of G-protein coupled receptors termed the orexin-1 (OX1) and orexin-2 (OX2) receptors. Emerging biology suggests the involvement of these receptors in psychiatric disorders as they are thought to play a key role in the regulation of multiple systems. This review is intended to highlight key selective OX1 or OX2 small-molecule antagonists.

Keywords: Hcrt-1; Hcrt-2; Hypocretin; Hypothalamus; Orexin.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Discovery
  • Humans
  • Hypothalamus / drug effects
  • Hypothalamus / metabolism
  • Intracellular Signaling Peptides and Proteins / metabolism
  • Neuropeptides / metabolism
  • Orexin Receptor Antagonists*
  • Orexin Receptors / metabolism
  • Orexins
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / pharmacology*

Substances

  • HCRT protein, human
  • Intracellular Signaling Peptides and Proteins
  • Neuropeptides
  • Orexin Receptor Antagonists
  • Orexin Receptors
  • Orexins
  • Small Molecule Libraries