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Discovery and evaluation of selective N-type calcium channel blockers: 6-Unsubstituted-1,4-dihydropyridine-5-carboxylic acid derivatives

  作者 Yamamoto, T; Niwa, S; Tokumasu, M; Onishi, T; Ohno, S; Hagihara, M; Koganei, H; Fujita, S; Takeda, T; Saitou, Y; Iwayama, S; Takahara, A; Iwata, S; Shoji, M  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-11;  页码  3639-3642  
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[摘要]A structure-activity relationship study of 6-unsubstituted-1,4-dihydropyridine and 2,6-unsubstituted-1,4-dihydropyridine derivatives was conducted in an attempt to discover N-type calcium channel blockers that were highly selective over L-type calcium channel blockers. Among the tested compounds, (+)-4-(3,5-dichloro-4-methoxy-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-cinnamyl ester was found to be an effective and selective N-type calcium channel blocker with oral analgesic potential. (C) 2012 Elsevier Ltd. All rights reserved.

 
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