enkephalinamide-leu--ala(2)- and beta-funaltrexamine

beta-FNA, the beta-fumaramate methyl ester of naltrexone, has been shown to antagonize irreversibly the actions of morphine on the guinea pig ileum and mouse vas deferens bioassays but does not affect the actions of delta-receptor ligands on the mouse vas deferens bioassay, suggesting that the compound does not irreversibly bind to the delta receptor. In this paper we examine the effect of beta-FNA on the binding of the prototypic delta agonists, Leu-enkephalin and D-Ala2-D-Leu5-enkephalin, its metabolically stable analogue, and show that treatment of membranes with beta-FNA does lead to alterations in the in vitro properties of delta receptors.

Topics: Animals; Brain; Cell Membrane; Enkephalin, Leucine; Enkephalin, Leucine-2-Alanine; Naloxone; Naltrexone; Oligopeptides; Protein Conformation; Rats; Receptors, Opioid