In the receptor-transducer model of pharmacological agonism, rejection of the traditional assumption that receptor molecules are in vast excess of transducer molecules permits the receptors to become distributed among unbound, bound and complexed states. Under these conditions, agonist affinities are liable to be overestimated when the method of irreversible receptor antagonism is used. Graphical tests have been developed to detect distribution, and these were applied to experimental data from the interaction between 5-HT and phenoxybenzamine on aortic tissue. Significant receptor distribution was not detected by the method. However, in the model it was assumed that there was a linear relation between the concentration of ternary complex and pharmacological effect. If this relation was replaced with a saturable one the effect of receptor distribution would be masked. The implications for pharmacologists and medicinal chemists are discussed.

中文翻译：

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激动剂亲和力估计的解释：分布受体状态的问题。

在药理学激动作用的受体-换能器模型中，对受体分子大大超过换能器分子的传统假设的拒绝允许受体在非结合状态，结合状态和复合状态之间分布。在这些条件下，当使用不可逆受体拮抗作用的方法时，激动剂亲和力易于被高估。已经开发出图形测试来检测分布，并将这些测试应用于主动脉组织上5-HT和苯氧基苯甲胺之间相互作用的实验数据。该方法未检测到明显的受体分布。但是，在该模型中，假定三元复合物的浓度与药理作用之间存在线性关系。如果这种关系被一个可饱和的关系所取代，那么受体分布的作用将被掩盖。讨论了对药理学家和药物化学家的意义。