Nagamatsu K, Kido Y, Terao T, Ishida T, Toki S
Life Sci. 1982 Oct 4;31(14):1451-7. doi: 10.1016/0024-3205(82)90006-6.
Specific binding of 3H-naloxone to opiate receptors was found to be irreversibly inactivated by morphine. This inactivation exhibited pseudo-first-order kinetics. The presence of sulfhydryl compounds or morphine during incubation with morphinone proved good protection. Morphinone-pretreated mice blocked the analgesic effect of morphine. The possible mechanism for these observations is proposed as follows: morphinone binds covalently to sulfhydryl group of opiate receptors, and inactivates irreversibly opiate binding sites, thus blocking the analgesic effect of morphine.
发现3H-纳洛酮与阿片受体的特异性结合被吗啡不可逆地失活。这种失活表现出假一级动力学。在与吗啡酮孵育期间存在巯基化合物或吗啡可提供良好的保护作用。经吗啡酮预处理的小鼠可阻断吗啡的镇痛作用。对这些观察结果的可能机制提出如下：吗啡酮与阿片受体的巯基共价结合，并不可逆地使阿片结合位点失活，从而阻断吗啡的镇痛作用。
