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不对称酯取代的1,4-二氢吡啶衍生物及其光学异构体对平滑肌收缩的影响。

Effects of unsymmetrical ester substituted 1,4-dihydropyridine derivatives and their optical isomers on contraction of smooth muscle.

作者信息

Towart R, Wehinger E, Meyer H

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1981 Sep;317(2):183-5. doi: 10.1007/BF00500079.

Abstract

The optical isomers of two nifedipine-like 1,4-dihydropyridine derivates have been synthesised and tested in vitro. The (-)-isomer (S-configuration of both compounds) was more potent than the racemate, which in turn was more potent than the (+)-isomer (R-configuration). The S-configuration isomers are approximately ten times more potent that nifedipine, and may represent the optimal structure and configuration for binding to and inhibiting calcium channels.

摘要

已合成两种硝苯地平样1,4 - 二氢吡啶衍生物的光学异构体并进行体外测试。(-)-异构体(两种化合物的S构型)比外消旋体更有效,而外消旋体又比(+)-异构体(R构型)更有效。S构型异构体的效力约为硝苯地平的十倍,可能代表与钙通道结合和抑制钙通道的最佳结构和构型。

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