Oxime derivatives related to AP18: Agonists and antagonists of the TRPA1 receptor

被引：45

作者：

DeFalco, Jeff ^{[1
]}

Steiger, Daniel ^{[1
]}

Gustafson, Amy ^{[1
]}

Emerling, Daniel E. ^{[1
]}

Kelly, Michael G. ^{[1
]}

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

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 01期

关键词：

TRPA1; TRP; Antagonist; Agonist; Transient Receptor Potential; Ankyrin-repeat Transient Receptor Potential 1; Oxime; AP18; NOCICEPTIVE NEURONS; CHANNEL; ACTIVATION; INFLAMMATION; PAIN;

D O I：

10.1016/j.bmcl.2009.10.113

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

AP18 1 was recently disclosed as an antagonist of the TRPA1 receptor by the research group of Patapoutian. However, no detailed structure-activity relationships around 1 have been disclosed. Thus, a small number of oximes related to AP18 were examined in order to characterize the determinants of TRPA1 activity. Congeners of AP18 were found to possess both agonist and antagonist activity, suggesting that AP18 may behave as a covalent antagonist of the TRPA1 ion-channel. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：276 / 279

页数：4

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