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在构效关系研究中,甾体类化合物的分配系数(Rm值)作为其亲脂性特征的一种表达。

Rm values of steroids as an expression of their lipophilic character in structure-activity studies.

作者信息

Biagi G L, Barbaro A M, Gandolfi O, Guerra M C, Cantelli-Forti G

出版信息

J Med Chem. 1975 Sep;18(9):873-83. doi: 10.1021/jm00243a003.

Abstract

The chromatographic Rm values of three series of steroids were determined by means of a reversed-phase system. The Rm values at 45% acetone in the mobile phase were shown to be correlated with the partition coefficients in an ether-water system. However, an almost equally good correlation was found when using extrapolated Rm values. The extrapolation technique could provide a standard system. The relationship between biological data and Rm values pointed out the important role of the lipophilic character in regulating the activity of steroids. In particular, the dependence of protein binding absorption and biotransformation on lipophilic character might strongly influence the availability of steroids at the site of action.

摘要

通过反相系统测定了三类甾体化合物的色谱比移值(Rm)。结果表明,流动相中丙酮含量为45%时的Rm值与在醚 - 水体系中的分配系数相关。然而,使用外推得到的Rm值时,也发现了几乎同样良好的相关性。外推技术可提供一个标准体系。生物学数据与Rm值之间的关系表明,亲脂性在甾体化合物活性调节中起重要作用。特别是,蛋白质结合、吸收和生物转化对亲脂性的依赖性可能会强烈影响甾体化合物在作用部位的可利用性。

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