Open AccessOrexin Receptor Antagonism: A New Principle in Neuroscience
Author(s) -
Christoph Boss,
Catherine BrisbareRoch,
F. Jenck,
Hamed Aissaoui,
Ralf Koberstein,
Thierry Sifferlen,
Thomas Weller
Publication year - 2008
Publication title -
chimia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.387
H-Index - 55
eISSN - 2673-2424
pISSN - 0009-4293
DOI - 10.2533/chimia.2008.974
Subject(s) - narcolepsy , orexin , neuroscience , alertness , orexin receptor , arousal , receptor , sleep (system call) , wakefulness , psychology , neuropeptide , medicine , neurology , pharmacology , electroencephalography , computer science , operating system
Orexins are hypothalamic neuropeptides interacting with G-protein coupled receptors in the brain. They play a role in the regulation of sleep–wake cycles in mammals, as suggested by the deficits in orexinergic function that are associated with rodent, canine and human narcolepsy. Selective or dual orexin1-receptor and/or orexin2-receptor antagonists or agonists that cross the blood-brain-barrier (BBB) may be of therapeutic interest for disorders of disturbed arousal and alertness. This article summarizes recent research to identify and characterize orexin receptor antagonists and their therapeutic potential for normalizing sleep in insomnia patients.