Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia

C Betschart, S Hintermann, D Behnke…

文献索引：Betschart, Claudia; Hintermann, Samuel; Behnke, Dirk; Cotesta, Simona; Fendt, Markus; Gee, Christine E.; Jacobson, Laura H.; Laue, Grit; Ofner, Silvio; Chaudhari, Vinod; Badiger, Sangamesh; Pandit, Chetan; Wagner, Juergen; Hoyer, Daniel Journal of Medicinal Chemistry, 2013 , vol. 56, # 19 p. 7590 - 7607

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被引用次数: 38

摘要

Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep disorders in several recent clinical trials in volunteers and primary insomnia patients. The relative contribution of antagonism of OX1R and OX2R for sleep induction is still a matter of debate. We therefore initiated a drug discovery project with the aim of creating both OX2R ...