Tetrahydroquinoline derivatives as opioid receptor antagonists

被引：8

作者：

Zhang, Cunyu ^{[1
]}

Westaway, Susan M. ^{[2
]}

Speake, Jason D. ^{[1
]}

Bishop, Michael J. ^{[1
]}

Goetz, Aaron S. ^{[3
]}

Carballo, Luz Helena ^{[3
]}

Hu, Mike ^{[4
]}

Epperly, Andrea H. ^{[4
]}

机构：

[1] GlaxoSmithKline, Dept Med Chem, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline, Immunoinflammat CEDD, Stevenage SG1 2NY, Herts, England

[3] GlaxoSmithKline, Mol Discovery Res, Screening & Compound Profiling, Res Triangle Pk, NC 27709 USA

[4] GlaxoSmithKline, Dept Drug Metab & Pharmacokinet, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 02期

关键词：

Tetrahydroquinoline; Opioid; Antagonist; NALOXONE; ANALOGS; RATS; FOOD;

D O I：

10.1016/j.bmcl.2010.12.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58 nM (K-i) functional activity against the mu opioid receptor. DMPK data suggest that novel tetrahydroquinoline analogs may be advantageous in peripheral applications. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：670 / 676

页数：7

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