Konno F, Shibata R, Takayanagi I, Hirobe M
J Pharmacobiodyn. 1984 Apr;7(4):221-6. doi: 10.1248/bpb1978.7.221.
We examined the interaction of morphine-epoxide, which was assumed to be a new metabolite of morphine, with opiate receptor subtypes using pharmacological and biochemical techniques. Morphine-epoxide was about 3 to 4 times less potent than morphine to the interactions of opiate receptors. However, the ratio of IC50 values for the guinea pig ileum and mouse vas deferens to electrical field stimulation and the ratio of IC50 values for the [3H]-dihydromorphine and [3H]-D-ala2-D-leu5 enkephalin binding to rat brain membrane preparations of morphine-epoxide was similar to those of morphine. Morphine-epoxide had virtually no effect on the twitch responses of rabbit and rat vas deferens. Furthermore, "sodium ratio" and "GTP ratio" of morphine-epoxide were similar to those of morphine and differed from naloxone. These results suggest that morphine-epoxide as well as morphine behaves as the agonist on the mu type opiate receptor notwithstanding that the affinity of morphine-epoxide is slightly less than that of morphine.
我们运用药理学和生物化学技术，研究了假定为吗啡新代谢产物的吗啡环氧化物与阿片受体亚型的相互作用。吗啡环氧化物对阿片受体相互作用的效力比吗啡低约3至4倍。然而，吗啡环氧化物对豚鼠回肠和小鼠输精管电场刺激的IC50值之比，以及对大鼠脑膜制剂中[3H]-二氢吗啡和[3H]-D-ala2-D-leu5脑啡肽结合的IC50值之比，与吗啡的相似。吗啡环氧化物对兔和大鼠输精管的抽搐反应几乎没有影响。此外，吗啡环氧化物的“钠比率”和“GTP比率”与吗啡的相似，与纳洛酮不同。这些结果表明，尽管吗啡环氧化物的亲和力略低于吗啡，但它与吗啡一样，在μ型阿片受体上表现为激动剂。
