通过放射性配体结合试验评估新型1,4 - 二氢吡啶衍生物SM - 6586及其异构体的钙拮抗作用。
Assessment of Ca(2+)-antagonistic effect of SM-6586 and its isomers, novel 1,4-dihydropyridine derivatives, by radioligand binding assay.
作者信息
Kinami J, Qu Y L, Tsuchihashi H, Nagatomo T, Maniwa T, Miyagishi A
机构信息
Department of Pharmacology, Niigata College of Pharmacy, Japan.
出版信息
Jpn J Pharmacol. 1992 Jan;58(1):75-8. doi: 10.1254/jjp.58.75.
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.
使用放射性配体结合试验，比较了1,4 - 二氢吡啶衍生物（±）SM - 6586及其光学异构体与它的两种衍生物（±）SM - 7297和（±）SM - 7548以及其他钙拮抗剂的钙拮抗作用。在大鼠脑和心脏中，SM - 6586光学异构体的钙拮抗作用顺序为：（+）＞（±）＞（ - ）SM - 6586。（+）SM - 6586的pKi值与尼莫地平、尼卡地平、硝苯地平和尼群地平的pKi值相当。（+）SM - 6586的pA2值在SM - 6586异构体中最高，因此表明（+）SM - 6586具有强大的钙拮抗作用。
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