Capetola R J, Gero A
Arch Int Pharmacodyn Ther. 1977 Feb;225(2):208-20.
Study of the interaction of 14-hydroxylated morphines and morphinans with human serum esterase revealed behavior similar to that of other morphine derivates as shown by similar acceleratory efficacies and affinity constants. However, 14-hydroxydihydro-6-morphinones showed anomalously low apparent affinities and anomalously high apparent efficacies, while at the same time seemingly interfering with the attachment of another drug to the enzyme. These anomalies are satisfactorily explained by assuming a second receptor site for which only the hydroxyketones have affinity and which interacts with the receptor site common to all opiates and opiate antagonists. Equations derived from this assumption allow to determine the parameters of the interactions of drugs with both receptor sites.
对14-羟基吗啡和吗啡喃与人血清酯酶相互作用的研究表明，其行为与其他吗啡衍生物相似，表现出相似的加速效能和亲和常数。然而，14-羟基二氢-6-吗啡酮表现出异常低的表观亲和力和异常高的表观效能，同时似乎会干扰另一种药物与该酶的结合。假设存在第二个受体位点，只有羟基酮对其有亲和力，且该位点与所有阿片类药物和阿片类拮抗剂共有的受体位点相互作用，这些异常现象就能得到满意的解释。基于这一假设推导的方程式可以确定药物与两个受体位点相互作用的参数。
