文章基本信息

标题：INTERACTION OF MORPHINE-EPOXIDE WITH MULTIPLE OPIATE RECEPTORS
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作者：FUKIO KONNO ; REIKO SHIBATA ; ISSEI TAKAYANAGI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1984
卷号：7
期号：4
页码：221-226
DOI：10.1248/bpb1978.7.221
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：multiple opiate receptor