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分配系数与生物学反应之间关系的动力学分析

Kinetic analysis of relationship between partition coefficient and biological response.

作者信息

Cooper E R, Berner B, Bruce R D

出版信息

J Pharm Sci. 1981 Jan;70(1):57-9. doi: 10.1002/jps.2600700110.

DOI:10.1002/jps.2600700110
PMID:7229930
Abstract

Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logarithm of the concentration for 50% receptor binding versus log P having a slope of greater than one. This result is in contrast to the equilibrium model for an initial slope of less than one. Thus, a criterion is established for deciding whether equilibrium or nonequilibrium processes apply.

摘要

非平衡模型和平衡模型都被提出来用以解释一组同系物相对于油水分配系数(P)的最佳生物学反应。对Hansch提出的动力学模型进行详细分析,结果表明该模型呈双线性形式,即50%受体结合时浓度的对数与log P的初始斜率大于1。这一结果与初始斜率小于1的平衡模型形成对比。因此,确立了一个用于判定适用平衡过程还是非平衡过程的标准。

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