Irreversible ligands with high selectivity toward delta and mu opiate receptors.
Alkylating agents that display strong selectivity for opiate receptor types delta or mu were prepared by appropriate modification of the structures of the strong analgesics fentanyl, etonitazene, and endoethenotetrahydrooripavine. The availability of these substances should facilitate studies of the structural basis of receptor specificity and of the physiologic roles of these receptors.
D000478:Alkylation; D000818:Animals; D001562:Benzimidazoles / Q000031:analogs & derivatives / Q000378:metabolism; D001921:Brain / Q000502:physiology; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002621:Chemistry; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives / Q000378:metabolism; D005283:Fentanyl / Q000031:analogs & derivatives / Q000378:metabolism; D017879:Isothiocyanates; D008024:Ligands; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism* / Q000502:physiology; D013797:Thebaine / Q000031:analogs & derivatives / Q000494:pharmacology
D001562:Benzimidazoles; D017879:Isothiocyanates; D008024:Ligands; D011957:Receptors, Opioid; D013797:Thebaine; D004744:Enkephalin, Methionine; C022118:enkephalinamide-Met, Ala(2)-; C037091:fentanyl isothiocyanate; C037669:endo-ethenotetrahydrooripavine; D005283:Fentanyl