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

被引：74

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

页码：898 / 903

页数：6

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