Peptide E: opiate receptor binding profile in the rat brain membrane assay. Comparison with beta-endorphin |
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| Authors: | M Westphal C H Li E P Heimer J Meienhofer |
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| Affiliation: | 1. Hormone Research Laboratory, University of California, San Francisco, CA 94143 USA;2. Bio-organic Chemistry Department, Roche Research Center, Hoffmann-La Roche Inc., Nutley, N. J. 07110 USA |
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| Abstract: | Beta-endorphin (beta-EP) and peptide E were compared in respect to their binding potency in the rat brain membrane by radioreceptor binding assay using tritiated human beta-EP, [D-Ala2,D-Leu5]-enkephalin (DADLE), dihydromorphine (DHM) and ethylketocyclazocine (EKC) as primary ligands. When the potency of beta h-EP was chosen to be 100%, peptide E was equipotent with beta-EP in displacing DHM (95%) and EKC (103%) less potent for competing with beta h-EP (60%) and least active (7%) for displacing DADLE. It may be concluded that peptide E binds preferentially with the opiate mu and kappa receptors in the rat brain membrane. |
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| Keywords: | human β-endorphin EK enkephalin HPLC high performance liquid chromatography DADLE DHM dihydromorphine EKC ethylketocyclazocine |
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