Assessment of Ca2+-Antagonistic Effects of SM-6586 and Its Isomers, Novel 1,4-Dihydropyridine Derivatives, by Radioligand Binding Assay.

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  • Assessment of Ca-antagonistic effects of SM-6586 and its isomers, novel 1,4-dihydropyridine derivatives, by radioligand binding assay

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The Ca2+-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 Ca2+-antagonists using a radioligand binding assay. The Ca2+-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 pA2 value for (+)SM-6586 was the highest among the SM-6586 isomers, thus suggesting that (+)SM-6586 has a potent Ca2+-antagonistic effect.

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