Irreversible ligands with high selectivity toward delta and mu opiate receptors

Science. 1983 Apr 15;220(4594):314-6. doi: 10.1126/science.6132444.

Abstract

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.

MeSH terms

  • Alkylation
  • Animals
  • Benzimidazoles / analogs & derivatives
  • Benzimidazoles / metabolism
  • Brain / physiology
  • Cells, Cultured
  • Chemical Phenomena
  • Chemistry
  • Enkephalin, Methionine / analogs & derivatives
  • Enkephalin, Methionine / metabolism
  • Fentanyl / analogs & derivatives
  • Fentanyl / metabolism
  • Isothiocyanates*
  • Ligands
  • Rats
  • Receptors, Opioid / metabolism*
  • Receptors, Opioid / physiology
  • Thebaine / analogs & derivatives
  • Thebaine / pharmacology

Substances

  • Benzimidazoles
  • Isothiocyanates
  • Ligands
  • Receptors, Opioid
  • Thebaine
  • Enkephalin, Methionine
  • enkephalinamide-Met, Ala(2)-
  • fentanyl isothiocyanate
  • endo-ethenotetrahydrooripavine
  • Fentanyl