title: Selective orexin receptor antagonists.
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.
authors.affiliation: Janssen Research & Development, 3210 Merryfield Row, San Diego, CA 92121, USA.
authors.forename: Terry P
authors.initials: TP
authors.lastname: Lebold
authors.forename: Pascal
authors.initials: P
authors.lastname: Bonaventure
authors.forename: Brock T
authors.initials: BT
authors.lastname: Shireman
mesh_terms: D000818:Animals; D055808:Drug Discovery; D006801:Humans; D007031:Hypothalamus / Q000187:drug effects / Q000378:metabolism; D047908:Intracellular Signaling Peptides and Proteins / Q000378:metabolism; D009479:Neuropeptides / Q000378:metabolism; D000068796:Orexin Receptor Antagonists; D064446:Orexin Receptors / Q000378:metabolism; D000068797:Orexins; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: C000596229:HCRT protein, human; D047908:Intracellular Signaling Peptides and Proteins; D009479:Neuropeptides; D000068796:Orexin Receptor Antagonists; D064446:Orexin Receptors; D000068797:Orexins; D054852:Small Molecule Libraries
keywords: Hcrt-1; Hcrt-2; Hypocretin; Hypothalamus; Orexin