Craig D A
Department of Biochemical Sciences, Wellcome Research Laboratories, Beckenham, Kent, UK.
Trends Pharmacol Sci. 1993 Mar;14(3):89-91. doi: 10.1016/0165-6147(93)90070-z.
For a variety of reasons, pharmacologists often construct 'inhibition curves' to evaluate antagonists rather than employing the more comprehensive 'Schild analysis'. There is a widespread perception that it is only possible to derive antagonist Kb values from such experiments via application of the Cheng-Prusoff equation, requiring knowledge of the agonist affinity at the receptor. In this article, Douglas Craig presents a practical examination of 'inhibition curve' methodology and demonstrates that it is a related equation requiring no knowledge of agonist affinity, rather than the Cheng-Prusoff equation, that affords theoretically valid estimates of antagonist Kb values from this technique.
由于多种原因，药理学家通常构建“抑制曲线”来评估拮抗剂，而不是采用更全面的“施尔德分析”。人们普遍认为，只有通过应用程-普鲁索夫方程，才能从这类实验中得出拮抗剂的Kb值，而这需要知道激动剂在受体上的亲和力。在本文中，道格拉斯·克雷格对“抑制曲线”方法进行了实际检验，并证明从该技术得出理论上有效的拮抗剂Kb值的是一个无需知道激动剂亲和力的相关方程，而非程-普鲁索夫方程。
