[Synthesis and pharmacological activities of the 1-substituted 4-methoxycarbonyl fentanyl derivatives].
Five derivatives of 4-methoxycarbonyl fentanyl were synthesized, four of them carry in the molecules some radicals that may alkylate opiate receptors. Their analgesic activities were measured and the irreversible inhibitory effects of all compounds on the electrically elicited contraction of MVD were investigated. The analgesic test showed that the compounds in this series possess analgesic activity with typical morphine--like action. The isolated tissue experiment indicated that these new compounds were all capable of binding with opiate receptors, and that compounds 2, 4 and 5 were determined to be a new irreversible ligand of opiate receptors.
Institute of Pharmaceutical Chemistry, PLA, Beijing.
M
M
Yi
G Z
GZ
Zhu
J G
JG
Li
J S
JS
Chen
D000701:Analgesics, Opioid / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D005260:Female; D005283:Fentanyl / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects; D014649:Vas Deferens / Q000187:drug effects
D000701:Analgesics, Opioid; D011957:Receptors, Opioid; C017114:carfentanil; D005283:Fentanyl