Calderone V, Martinotti E
Dipartimento di Psichiatria, Neurobiologia, Farmacologia, e Biotecnologie, Università degli Studi di Pisa, Italy.
J Pharmacol Toxicol Methods. 1998 Jul;40(1):57-62. doi: 10.1016/s1056-8719(98)00039-2.
The estimation of the dissociation constant (Ka) of full agonists represents an essential tool for the classification of drugs and drug receptors, in functional pharmacology. The evaluation of the Ka was a problem until the development of the Furchgott's method (irreversible partial receptor inactivation method), which surely represents the most used analysis for the evaluation of the agonist Ka in experimental protocols on isolated tissues. The Furchgott's method can furnish a reliable estimation of the Ka, but it requires a relatively complicated manipulation of experimental data. In this article, an alternative approach for the evaluation of the Ka is proposed, on the basis of empirical considerations. This method, also based on the partial alkylation of a fraction of receptors, needs only the knowledge of the location parameters of the concentration-response curves and the application of a very simple equation, without any complicated intermediate interpolation of the experimental data.
在功能药理学中，对完全激动剂解离常数（Ka）的估计是药物和药物受体分类的重要工具。在弗奇戈特方法（不可逆部分受体失活法）出现之前，Ka的评估一直是个问题，该方法无疑是在离体组织实验方案中评估激动剂Ka时最常用的分析方法。弗奇戈特方法能够提供可靠的Ka估计值，但它需要对实验数据进行相对复杂的处理。本文基于经验考虑，提出了一种评估Ka的替代方法。该方法同样基于部分受体的烷基化，只需要知道浓度-反应曲线的定位参数并应用一个非常简单的方程，无需对实验数据进行任何复杂的中间插值。
