Vere D W
J Pharmacol Exp Ther. 1978 Jun;205(3):617-23.
The methods which exist to represent agonist-antagonist interactions, and to distinguish between them are sufficient and effective. Their effective use depends on a set of criteria which are not always fulfilled in actual experiments. In some situations it is difficult or impossible to meet these criteria. An alternative representation is proposed, using straightforward geometry, which evades this problem. It also allows experimental data points to be selected without bias and makes it possible to apply orthodox criteria to more restricted sets of data than is otherwise the case. To do this, it is necessary to reverse the ordinary procedure in antagonist assays, by adding successive concentrations of antagonist to a preparation so that a constant response is evoked by squared multiples of the original agonist dose. This can only be done with rapidly reversible antagonists, but the method has been shown to be effective for such drugs.
现有的表示激动剂 - 拮抗剂相互作用并区分它们的方法是充分且有效的。它们的有效使用取决于一组标准，而这些标准在实际实验中并非总能得到满足。在某些情况下，很难或不可能满足这些标准。本文提出了一种使用直观几何图形的替代表示方法，该方法避免了这个问题。它还允许无偏差地选择实验数据点，并使得能够将正统标准应用于比其他情况更受限的数据组。为此，有必要颠倒拮抗剂测定中的常规程序，即向制剂中逐次添加拮抗剂浓度，以便通过原始激动剂剂量的平方倍数引发恒定反应。这只能用快速可逆的拮抗剂来完成，但该方法已被证明对这类药物有效。
