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

Selective orexin receptor antagonists.

Author information

1
Janssen Research & Development, 3210 Merryfield Row, San Diego, CA 92121, USA.

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

PMID:
23891187
DOI:
10.1016/j.bmcl.2013.06.057
[Indexed for MEDLINE]

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