Venter D P
Department of Pharmacology, Potchefstroom University for Christian Higher Education, South Africa.
Eur J Pharmacol. 1997 Feb 12;320(2-3):223-31. doi: 10.1016/s0014-2999(96)00899-0.
A new method for estimating relative efficacies and relative intrinsic efficacies of agonists is described. Relative efficacy is estimated by employing a newly defined efficacy related parameter (eES) and it may be estimated without prior knowledge of efficacy values or the value of the equilibrium dissociation constants, KA, of agonist-receptor complexes. The parameter eES is directly related to efficacy (e) and is defined as the ratio of maximal stimulus to maximal effect of an agonist. The value of eES indicates whether or not spare receptors are present for a particular agonist-effector system. The eES values of agonists are estimated by utilizing submaximal concentration-effect curves determined with fixed agonist-competitive antagonist concentration combinations and choosing a suitable reference (height of an agonistic concentration-effect curve) to which the height of the stimulus concentration-effect curves of the agonist may be compared. In addition to eES, other new agonist-effector parameters, namely SEm/Sm and phi min, were also defined.
描述了一种估算激动剂相对效能和相对内在效能的新方法。通过使用新定义的与效能相关的参数（eES）来估算相对效能，并且无需事先了解效能值或激动剂-受体复合物的平衡解离常数KA的值即可进行估算。参数eES与效能（e）直接相关，定义为激动剂的最大刺激与最大效应之比。eES的值表明特定激动剂-效应器系统是否存在备用受体。通过利用固定激动剂-竞争性拮抗剂浓度组合测定的次最大浓度-效应曲线，并选择合适的参考值（激动剂浓度-效应曲线的高度）与激动剂刺激浓度-效应曲线的高度进行比较，来估算激动剂的eES值。除了eES之外，还定义了其他新的激动剂-效应器参数，即SEm/Sm和phi min。
