Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3)

被引：14
|
作者：
Kuduk, Scott D. [1 ]
Chang, Ronald K. [1 ]
Di Marco, Christina N. [1 ]
DiPardo, Robert M. [1 ]
Cook, Sean P. [2 ]
Cato, Matthew J. [2 ]
Jovanovska, Aneta [2 ]
Urban, Mark O. [2 ]
Leitl, Michael [2 ]
Spencer, Robert H. [2 ]
Kane, Stefanie A. [2 ]
Hartman, George D. [1 ]
Bilodeau, Mark T. [1 ]
机构：
[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA
[2] Merck Res Labs, Dept Pain Res, West Point, PA 19486 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 14期
关键词：
ASIC3; Pain; Non-amidine; Blood-to-plasma; A-317567; AMYGDALA; SENSORS; FEAR;
D O I：
10.1016/j.bmcl.2011.05.064
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of benzothiophene methyl amines were examined in an effort to identify non-amidine chemotypes with reduced polypharmacology from existing leads with the goal of finding potent ASIC3 channel blockers to advance the therapeutic evaluation of ASIC3 inhibition. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4255 / 4258
页数：4
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