THE CHENG-PRUSOFF RELATIONSHIP - SOMETHING LOST IN THE TRANSLATION
THE CHENG-PRUSOFF RELATIONSHIP - SOMETHING LOST IN THE TRANSLATION
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DOI：
10.1016/0165-6147(93)90070-z
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发表时间：
1993-03-01
影响因子：
13.8
通讯作者：
CRAIG, DA
中科院分区：
文献类型：
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作者：
CRAIG, DA
由于各种原因，药理学家经常构建“抑制曲线”来评估拮抗剂，而不是采用更全面的“Schild分析”。人们普遍认为，只有通过应用Cheng-Prusoff方程才能从这些实验中推导出拮抗剂K（B）值，这需要了解受体上的激动剂亲和力。在这篇文章中，道格拉斯克雷格提出了一个实际检查的“抑制曲线”的方法，并证明这是一个相关的方程，而不是郑-普鲁索夫方程，不需要知识的激动剂亲和力，提供理论上有效的估计拮抗剂K（B）值从这种技术。
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 K(b) 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 K(b) values from this technique.