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Effect of β‐FNA on Opiate δ Receptor Binding
Author(s) -
Rothman Richard B.,
Schumacher Uwe K.,
Pert Candace B.
Publication year - 1984
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1984.tb12861.x
Subject(s) - opiate , opiate receptors , receptor , medicine , chemistry , pharmacology , opioid , (+) naloxone
(β‐FNA, the β ‐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 δ‐receptor ligands on the mouse vas deferens bioassay, suggesting that the compound does not irreversibly bind to the S receptor. In this paper we examine the effect of (β ‐FNA on the binding of the prototypic δ agonists, Leuenkephalin and d ‐Ala 2 ‐ d ‐Leu 5 ‐enkephalin, its metabolically stable analogue, and show that treatment of membranes with β ‐FNA does lead to alterations in the in vitro properties of δ receptors.