Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type1 Selective Antagonist

被引：73
|
作者：
Steiner, Michel A. [1 ]
Gatfield, John [1 ]
Brisbare-Roch, Catherine [1 ]
Dietrich, Hendrik [1 ]
Treiber, Alexander [1 ]
Jenck, Francois [1 ]
Boss, Christoph [1 ]
机构：
[1] Actel Pharmaceut Ltd, CH-4123 Allschwil, Switzerland
来源：
CHEMMEDCHEM | 2013年 / 8卷 / 06期
关键词：
anxiety; neurotransmitters; orexin receptor antagonists; peptides; sleep; SLEEP; PROMOTION; SYSTEM;
D O I：
10.1002/cmdc.201300003
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Stress relief: Orexin neuropeptides regulate arousal and stress processing through orexin receptor type1 (OXR-1) and 2 (OXR-2) signaling. A selective OXR-1 antagonist, represented by a phenylglycine-amide substituted tetrahydropapaverine derivative (ACT-335827), is described that is orally available, penetrates the brain, and decreases fear, compulsive behaviors and autonomic stress reactions in rats. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
引用
收藏
页码：898 / 903
页数：6
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