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  • Title: Evidence that the delta-selective alkylating agent, fit, alters the mu-noncompetitive opiate delta binding site.
    Author: Rothman RB, Danks JA, Herkenham M, Jacobson AE, Burke TR, Rice KC.
    Journal: Neuropeptides; 1985 Jun; 6(3):227-37. PubMed ID: 2991807.
    Abstract:
    Considerable evidence supports the notion that the prototypic delta agonist [3H]D-ala2-D-leu5-enkephalin labels two binding sites on brain membranes in vitro. Recent studies have demonstrated that treatment of brain membranes with the delta-selective, site-directed, alkylating agent, FIT (Rice et al., Science 220, 314-316, 1983) results in a membrane preparation devoid of detectable higher affinity [3H]D-ala2-D-leu5-enkephalin binding sites, but contain residual lower affinity binding sites at which mu-ligands are apparent noncompetitive inhibitors (Rothman et al., Neuropeptides 4:210-215, 1984). In this paper we extend these data by showing that although FIT eliminates the higher affinity binding site, it also alters the properties of the residual lower affinity binding sites.
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