TY - JOUR AU - Boss, Christoph AU - Brisbare-Roch, Catherine AU - Jenck, Francois AU - Aissaoui, Hamed AU - Koberstein, Ralf AU - Sifferlen, Thierry AU - Weller, Thomas PY - 2008/12/17 Y2 - 2024/03/29 TI - Orexin Receptor Antagonism: A New Principle in Neuroscience JF - CHIMIA JA - Chimia VL - 62 IS - 12 SE - Scientific Articles DO - 10.2533/chimia.2008.974 UR - https://www.chimia.ch/chimia/article/view/2008_974 SP - 974 AB - 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. ER -