Journal
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 51, 2011
Volume 51, Issue -, Pages 243-266Publisher
ANNUAL REVIEWS
DOI: 10.1146/annurev-pharmtox-010510-100528
Keywords
hypocretin; insomnia; hypnotic; sedative; narcolepsy; substance abuse
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Funding
- NHLBI NIH HHS [P01 HL095491, HL095491, P01 HL095491-02] Funding Source: Medline
- NINDS NIH HHS [R01 NS055367, NS055367, R01 NS055367-09] Funding Source: Medline
- NATIONAL HEART, LUNG, AND BLOOD INSTITUTE [P01HL095491] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE [R01NS055367] Funding Source: NIH RePORTER
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Orexin-A and -B (also known as hypocretin-1 and -2) are neuropeptides produced in the lateral hypothalamus that promote many aspects of arousal through the OX1 and OX2 receptors. In fact, they are necessary for normal wakefulness, as loss of the orexin-producing neurons causes narcolepsy in humans and rodents. This has generated considerable interest in developing small-molecule orexin receptor antagonists as a novel therapy for the treatment of insomnia. Orexin antagonists, especially those that block OX2 or both OX1 and OX2 receptors, clearly promote sleep in animals, and clinical results are encouraging: Several compounds are in Phase III trials. As the orexin system mainly promotes arousal, these new compounds will likely improve insomnia without incurring many of the side effects encountered with current medications
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