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- W1982485725 abstract "[3H]ET (etorphine), which is considered either as an “universal” ligand or a μ agonist, interacts with identical affinities KD = 0.33 – 0.38 nM to hybrid cells and rabbit cerebellum, pure δ and μ-enriched opioid receptor preparations, respectively. In rat brain tissue, [3H]ET binding is inhibited by DAGO (Tyr-D-Ala-Gly-(Me)-Phe-Gly-ol), a μ selective agonist, in a competitive manner without apparent modification of the maximal number of sites. Furthermore, even at a DAGO concentration (300 nM) which should be sufficient to block [3H]ET interaction with μ sites, no variation in the total capacity of the tritiated ligand is observed. In contrast, DTLET (Tyr-D-Thr-Gly-Phe-Leu-Thr), a δ-preferential agonist, blocks [3H]ET binding in rat brain at a concentration able to saturate δ-sites. At higher concentrations, where DTLET cross reacts with μ-sites, this ligand exhibits similar properties to those of DAGO. These data are very different from those obtained with [3H]EKC (ethylketocyclazocine), another “universal” ligand, the binding properties of which are easily explained by the occurence in rat brain tissue of independent sites exhibiting pharmacological profiles of μ, δ and κ sites. Our results underline the possible misinterpretation of binding data obtained by using [3H] etorphine as a non selective ligand." @default.
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- W1982485725 date "1987-08-01" @default.
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- W1982485725 title "Differences of binding characteristics of non-selective opiates towards μ and δ receptor types" @default.
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- W1982485725 doi "https://doi.org/10.1016/0024-3205(87)90452-8" @default.
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