Calderone V
Istituto Policattedra di Discipline Biologiche, Facoltà di Farmacia, Università degli Studi di Pisa, Italy.
J Pharmacol Toxicol Methods. 1998 Apr;39(3):129-35. doi: 10.1016/s1056-8719(98)00013-6.
The Schild analysis is certainly the most reliable method for antagonism studies. The Schild regression allows one to determine the parameter of the Schild-slope, which represents a powerful diagnostic tool when investigating the nature of an antagonist and, consequently, to evaluate its potency. Nevertheless, in functional pharmacology, often practical reasons lead the experimenter to obtain an inhibition curve for the antagonist and calculate its potency by means of equations, which can be considered as a derivation of the Cheng-Prusoff analysis. This approach is considered theoretically invalid, because it does not allow to know the exact nature of the antagonism, and thus the evaluation of the antagonist dissociation constant can be meaningless. In this paper, a new method is proposed, which, by means of an equation closely similar to the Schild one, permits one to obtain a linear regression analysis, giving a slope value absolutely equivalent to the Schild-slope. This method allows us to determine both the nature and the potency of an antagonist, and requires an experimental procedure substantially analogous to the one performed to obtain an inhibition curve.
希尔德分析无疑是拮抗作用研究中最可靠的方法。希尔德回归使人们能够确定希尔德斜率参数，在研究拮抗剂的性质时，这是一个强大的诊断工具，从而能够评估其效力。然而，在功能药理学中，实际原因常常导致实验者获得拮抗剂的抑制曲线，并通过方程计算其效力，这些方程可被视为程-普鲁索夫分析的一种衍生方法。这种方法在理论上被认为是无效的，因为它无法确定拮抗作用的确切性质，因此对拮抗剂解离常数的评估可能毫无意义。本文提出了一种新方法，该方法通过一个与希尔德方程非常相似的方程，能够进行线性回归分析，得出的斜率值与希尔德斜率完全等效。这种方法使我们能够确定拮抗剂的性质和效力，并且所需的实验步骤与获取抑制曲线的实验步骤基本类似。
