Goodford P J, St-Louis J, Wootton R
Br J Pharmacol. 1980 Apr;68(4):741-8. doi: 10.1111/j.1476-5381.1980.tb10867.x.
1 The release of bound oxygen from oxyhaemoglobin by allosteric effectors is considered as a model for those drug-receptor interactions where the primary response to agonist binding is the release of a second messenger species. 2 A theory of haemoglobin oxygenation, based on the two-state model of Monod, Wyman & Changeux (1965) is used to predict the relationship between 'pharmacological' response and dose of agonist. This relationship is the same as that derived from classical pharmacological occupancy theory. 3 The potency of an agonist is a weighted average of its affinities for the two conformational states of the receptor. 4 The efficacy of an agonist depends not only upon its binding to one of the two conformational states, but also on its ability to alter the functional properties of that state by lowering the affinity of the state for the second messenger. 5 2,3-Diphosphoglycerate and adenosine triphosphate are approximately equipotent and of similar efficacy, but inositol hexaphosphate is about 500 times more potent and has a higher efficacy.
变构效应剂促使氧合血红蛋白释放结合氧，这被视为一种药物 - 受体相互作用的模型，在这种相互作用中，激动剂结合的主要反应是释放第二信使物质。
基于莫诺德、怀曼和尚热（1965年）的双态模型的血红蛋白氧合理论，用于预测“药理”反应与激动剂剂量之间的关系。这种关系与从经典药理占据理论得出的关系相同。
激动剂的效能是其对受体两种构象状态亲和力的加权平均值。
激动剂的效力不仅取决于其与两种构象状态之一的结合，还取决于其通过降低该状态对第二信使的亲和力来改变该状态功能特性的能力。
2,3 - 二磷酸甘油酸和三磷酸腺苷效力大致相当且功效相似，但肌醇六磷酸的效力约高500倍且功效更高。
