Journal article

Orexin OX2 Receptor Antagonists as Sleep Aids

Laura H Jacobson, Sui Chen, Sanjida Mir, Daniel Hoyer, AJ Lawrence (ed.), L DeLecea (ed.)

Current topics in behavioral neurosciences | SPRINGER INTERNATIONAL PUBLISHING AG | Published : 2017


The discovery of the orexin system represents the single major progress in the sleep field of the last three to four decades. The two orexin peptides and their two receptors play a major role in arousal and sleep/wake cycles. Defects in the orexin system lead to narcolepsy with cataplexy in humans and dogs and can be experimentally reproduced in rodents. At least six orexin receptor antagonists have reached Phase II or Phase III clinical trials in insomnia, five of which are dual orexin receptor antagonists (DORAs) that target both OX1 and OX2 receptors (OX2Rs). All clinically tested DORAs induce and maintain sleep: suvorexant, recently registered in the USA and Japan for insomnia, represent..

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