期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 6, 页码 1692-1696出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.089
关键词
T-type calcium channel; Structure-activity relationships; Pregnane X receptor; Electrocorticogram; Epilepsy
A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep. (C) 2011 Elsevier Ltd. All rights reserved.
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