PA2 AND RECEPTOR DIFFERENTIATION - STATISTICAL-ANALYSIS OF COMPETITIVE ANTAGONISM

被引:525
作者
TALLARIDA, RJ
COWAN, A
ADLER, MW
机构
[1] Department of Pharmacology Temple University School of Medicine Philadelphia
关键词
D O I
10.1016/0024-3205(79)90505-8
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
The pA2 of a competitive antagonist was defined by Schild as the negative logarithm of the molar concentration of an antagonist which reduces the effect of a dose of agonist to that of half the dose. The relationship of the pA2 to the dissociation constant, K, of the antagonist-receptor complex is discussed within the framework of competitive theory. Various methods for the determination of pA2, and the accuracy and precision of these methods, are presented. Special problems associated with the determination of pA2 in vivo are also discussed, with particular attention being given to narcotic analgesics and their antagonists. © 1979.
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页码:637 / 654
页数:18
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