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药理学中关于药物与受体相互作用的 Easson-Stedman 模式问世已60年了,其实用价值已被许多事实所肯定。但是这样的一个三点接触模式仍有许多不足或局限性,为使其更切实际,作者使用键合反应和手性识别机理对其进行了修正,提出以下四点建议:(1)配位体应被看作一个立体电子学药效基团;(2)数个相互反应点中的一个可以是相斥的;(3)药物与受体反应的功能团之键合能合并可使该模式用于定量;(4)发生在激活步骤的手性识别,可以把其中的一个部位看成启动/催化基团。
The pharmacological Esson-Stedman model of drug-receptor interaction has been around for 60 years, and its utility has been affirmed by many facts. However, there are still many deficiencies or limitations in such a three-point contact mode. To make it more realistic, the authors modify the mechanism by using the bonding reaction and chiral recognition mechanism. The following four suggestions are made: (1) Coordination The body should be considered as a stereoscopic electron-pharmacophore; (2) one of the several reaction sites may be repulsive; (3) the binding of the drug-receptor functional group can be combined Mode for quantification; and (4) chiral recognition that occurs at the activation step, one of which can be considered as a starter / catalyst group.