Assessment of Ca2+-Antagonistic Effects of SM-6586 and Its Isomers, Novel 1,4-Dihydropyridine Derivatives, by Radioligand Binding Assay.
- 1 January 1992
- journal article
- research article
- Published by Elsevier in The Japanese Journal of Pharmacology
- Vol. 58 (1) , 75-78
- https://doi.org/10.1254/jjp.58.75
Abstract
The Ca(2+)-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(2+)-antagonists using a radioligand binding assay. The Ca(2+)-antagonistic effects of the optical isomers of SM-6586 were in the order of (+) greater than (+/-) greater than (-)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 Ca(2+)-antagonistic effect.Keywords
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