☆ 4.5 Article

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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷 20, 期 12, 页码 3573-3578

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2010.04.125

关键词

Calcium-activated potassium channel; BKCa; BKCa agonists

类别

Chemistry, Medicinal Chemistry, Organic

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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.

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