4-甲氧羰基芬太尼1-位衍生物的合成及生物活性

SYNTHESIS AND PHARMACOLOGICAL ACTIVITIES OF THE 1-SUBSTITUTED 4-METHOXYCARBONYL FENTANYL DERIVATIVES

合成了5个4-甲氧羰基芬太尼1-位衍生物,有4个化合物的分子中带有可与阿片受体发生烷化反应的官能团。镇痛试验结果表明,它们都有典型的吗啡样镇痛活性。离体组织试验结果表明,这些新化合物均作用于阿片受体,其中化合物2,4和5为新型的阿片受体不可逆配体。

Five derivatives of 4-methoxycarbonyl fentanyl were synthesized, four of themcarry in the molecules some radicals that may alkylate opiate receptors. Their analgesic activities weremeasured and the irreversible inhibitory effects of all compounds on the electrically elicited contractionof MVD were investigated. The analgesic test showed that the compounds in this series possess analgesicactivity with typical morphine--like action. The isolated tissue experiment indicated that these newcompounds were all capable of binding with opiate receptors, and that compounds 2, 4 and 5 weredetermined to be a new irreversible ligand of opiate receptors.