Assessment of Ca<SUP>2+</SUP>-Antagonistic Effects of SM-6586 and Its Isomers, Novel 1, 4-Dihydropyridine Derivatives, by Radioligand Binding Assay
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概要
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The Ca<SUP>2+</SUP>-antagonistic effects of the 1, 4-dihydropyridine derivative (±)SM-6586 and its optical isomers were compared with those of its two derivatives ((±)SM-7297 and (±)SM-7548) and other Ca<SUP>2+</SUP>-antagonists using a radioligand binding assay. The Ca<SUP>2+</SUP>-antagonistic effects of the optical isomers of SM-6586 were in the order of (+) > (±) > (−)SM-6586 in both rat brain and heart. The pKi value of (+)SM-6586 was comparable to those of nimodipine, nicardipine, nifedipine and nitrendipine. The pA<SUB>2</SUB> value for (+)SM-6586 was the highest among the SM-6586 isomers, thus suggesting that (+)SM-6586 has a potent Ca<SUP>2+</SUP>-antagonistic effect.
著者
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Miyagishi Akira
Research Center Sumitomo Pharmaceuticals Co. Ltd
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Kinami Junji
Department Of Pharmacology Niigata College Of Pharmacy
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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Maniwa Takashi
Research Laboratories, Sumitomo Pharmaceuticals Co. Ltd.
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Qu Ying-Li
Department of Pharmacology, Niigata College of Pharmacy
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