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  • Title: Opiate receptor binding characteristics of dimeric analogues of mu-selective DAGO-enkephalin.
    Author: Shimohigashi Y, Waki M, Izumiya N, Costa T, Herz A, Kurono M, Yagi K.
    Journal: Biochem Int; 1986 Aug; 13(2):199-203. PubMed ID: 3021160.
    Abstract:
    DAGO-enkephalin ([ D-Ala2, MePhe4, Gly-ol5]enkephalin), a highly selective ligand for mu opiate receptors, was dimerized with a series of alpha,omega-alkanedioic acids (n = 2-12) at the OH-terminus. In the radioligand receptor binding assays with rat brain, most of the DAGO-enkephalin dimers with cross-linking methylene chain n (DEDn) were more potent than DAGO monomer. For delta receptors, affinity of DEDn was maximized with n = 8, which might be related to an optimal distance between two binding sites. For mu receptors, an increase in chain length resulted in a progressive loss of potency. Although all of DEDn are considerably mu-selective, with a mu/delta ratio of 15-50, DEDn exhibited fairly flat binding curves with 15-50% smaller sloped than that of DAGO, suggesting that the dimers interact more strongly with one of the possible two mu binding sites.
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