Structure-activity relationship (SAR) investigations of tetrahydroquinolines as BKCa agonists

被引：35
|
作者：
Gore, Vijay K. [1 ]
Ma, Vu V. [1 ]
Yin, Ruoyuan [2 ]
Ligutti, Joe [2 ]
Immke, David [2 ]
Doherty, Elizabeth M. [1 ]
Norman, Mark H. [1 ]
机构：
[1] Amgen Inc, Dept Chem Res & Discovery, Thousand Oaks, CA 91320 USA
[2] Amgen Inc, Dept Neurosci, Thousand Oaks, CA 91320 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 12期
关键词：
Calcium-activated potassium channel; BKCa; BKCa agonists; SMOOTH-MUSCLE; CHANNEL; MODULATION; OPENER;
D O I：
10.1016/j.bmcl.2010.04.125
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The membrane bound large-conductance, calcium-activated potassium channel (BKCa) is an important regulator of neuronal activity. Here we describe the identification and structure-activity relationship of a novel class of potent tetrahydroquinoline BKCa agonists. An example from this class of BKCa agonists was shown to depress the spontaneous neuronal discharges in an electrophysiological model of migraine. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3573 / 3578
页数：6
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