ASSESSMENT OF CA2+-ANTAGONISTIC EFFECTS OF SM-6586 AND ITS ISOMERS, NOVEL 1,4-DIHYDROPYRIDINE DERIVATIVES, BY RADIOLIGAND BINDING ASSAY

被引：6

作者：

KINAMI, J ^{[1
]}

QU, YL ^{[1
]}

TSUCHIHASHI, H ^{[1
]}

NAGATOMO, T ^{[1
]}

MANIWA, T ^{[1
]}

MIYAGISHI, A ^{[1
]}

机构：

[1] SUMITOMO PHARMACEUT CO LTD,RES LABS,OSAKA 554,JAPAN

来源：

JAPANESE JOURNAL OF PHARMACOLOGY | 1992年 / 58卷 / 01期

关键词：

D O I：

10.1254/jjp.58.75

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

页码：75 / 78

页数：4

共 8 条

[1] SOME QUANTITATIVE USES OF DRUG ANTAGONISTS [J].