Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)

被引：6

作者：

Gowlugari, Sumithra ^{[1
]}

DeFalco, Jeff ^{[1
]}

Nguyen, Margaret T. ^{[1
]}

Kaub, Carl ^{[1
]}

Chi, Candace ^{[1
]}

Duncton, Matthew A. J. ^{[1
]}

Emerling, Daniel E. ^{[1
]}

Kelly, Michael G. ^{[1
]}

Kincaid, John ^{[1
]}

Vincent, Fabien ^{[1
]}

机构：

[1] Renovis Inc, San Francisco, CA 94080 USA

来源：

MEDCHEMCOMM | 2012年 / 3卷 / 10期

关键词：

SELECTIVITY; ANANDAMIDE; MECHANISMS; ANALGESIA; SYSTEM;

D O I：

10.1039/c2md20146a

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Fatty acid amide hydrolase (FAAH) inhibition is a promising target for the treatment of pain, anxiety and depression. The vast majority of FAAH inhibitors contain an electrophilic moiety and are known to react covalently with the enzyme. Herein we present the discovery of potent inhibitors, such as RN-450 29, which are based upon a novel tetrahydropyridopyridine scaffold lacking an obvious electrophilic site, and which appear to inhibit FAAH in a reversible and non-covalent manner.

引用

页码：1258 / 1263

页数：6

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