部分激动剂的简单pA2估计：与考曼-布林克斯方法的比较。

Simple pA2 estimation of partial agonists: comparison with the Kaumann-Blinks method.

作者信息

Pöch G, Zimmermann I

机构信息

Institut für Pharmakodynamik und Toxikologie, Karl-Franzens-Universität Graz, Austria.

出版信息

J Pharmacol Methods. 1988 Mar;19(1):47-56. doi: 10.1016/0160-5402(88)90044-7.

DOI:10.1016/0160-5402(88)90044-7

PMID:3367648

Abstract

Estimation of KB and pA2 of partial agonists as antagonists of full agonists is hindered by their stimulant component of action. This reflects competitive synergism, i.e., an additive interaction with a full agonist. The antagonistic component of a partial agonist is seen as a parallel shift of the agonist curve to the right from a constructed additive dose-response curve, from which a dose ratio (DR) was determined for calculation of graphic estimation of KB or pA2 of partial agonists. Dose-response curves from eight studies were analyzed in this way, in comparison with the method of Kaumann and Blinks, and showed excellent agreement between pA2 values determined by either method (r = 0.994, slope = 0.999, n = 17).

摘要

将部分激动剂作为完全激动剂的拮抗剂来估算其KB和pA2，会受到其激动作用成分的阻碍。这反映了竞争性协同作用，即与完全激动剂的相加相互作用。部分激动剂的拮抗成分表现为激动剂曲线从构建的相加剂量-反应曲线向右平行移动，据此确定剂量比（DR）以计算部分激动剂的KB或pA2的图形估算值。以这种方式分析了八项研究的剂量-反应曲线，并与考曼和布林克斯的方法进行比较，结果表明两种方法所测定的pA2值之间具有极好的一致性（r = 0.994，斜率 = 0.999，n = 17）。