Discovery and evaluation of selective N-type calcium channel blockers: 6-unsubstituted-1,4-dihydropyridine-5-carboxylic acid derivatives |
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| Authors: | Yamamoto Takashi Niwa Seiji Tokumasu Munetaka Onishi Tomoyuki Ohno Seiji Hagihara Masako Koganei Hajime Fujita Shin-ichi Takeda Tomoko Saitou Yuki Iwayama Satoshi Takahara Akira Iwata Seinosuke Shoji Masataka |
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| Institution: | Exploratory Research Laboratories, Ajinomoto Pharmaceuticals Co. Ltd, Kawasaki-ku, Kawasaki-shi, Kanagawa, Japan. takashia_yamamoto@ajinomoto.com |
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| Abstract: | 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. |
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