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Spectrum of the mu binding sites delta binding sites and kappa binding sites in homogenates of rat brain


, : Spectrum of the mu binding sites delta binding sites and kappa binding sites in homogenates of rat brain. British Journal of Pharmacology 77(3): 461-468

In homogenates of rat brain, the binding characteristics of tritiated opiates and opioid peptides were examined and the relative capacities of .mu.-, .delta.- and .kappa.-binding sites of the opiate receptor were determined by saturation analysis. In competition experiments, binding of the selective .mu.-ligand [3H]-[D-Ala2,MePhe4,Gly-ol5]enkephalin at the .mu.-site was displaced by [D-Ala2,D-Leu5]enkephalin with rather low affinity (KI [inhibition constant] = 12.6 nM) and more readily by the ketazocine-like compounds (-)-ethylketazocine (KI = 3.1 nM) and (-)-bremazocine (KI = 0.32 nM), which also displaced the binding of [3H]-[D-Ala2,D-Leu5]enkephalin from the .delta.-site. The binding to the .kappa.-site was easily displaced by ethylketazocine (1.0 nM) and bremazocine (0.37 nM) but not by the .mu.-ligand [D-Ala2,MePhe4,Gly-ol5]enkephalin (KI = 2000-3000 nM) or the .delta.-ligand [D-Ala2,D-Leu5]enkephalin (KI > 20,000 nM). Kd and the binding capacity (pmol/g) of the .mu.-binding site were determined with the selective .mu.-ligand [3H]-[D-Ala2,MePhe4,Gly-ol5]enkephalin. For the .delta.-site, [3H]-[D-Ala2, D-Leu5]enkephalin was used in the presence of unlabeled [D-Ala2,MePhe4,Gly-ol5]enkephalin in order to suppress cross-reactivity to the .mu.-binding site. For the estimation of .delta.-binding, [3H]-(.+-.)-ethylketazocine or [3H]-(-)-bremazocine were used in the presence of unlabeled .mu.- and .delta.-ligands for the suppression of cross-reactivities to the .mu.- and .delta.-binding sites. In rat brain the capacity of the .mu.-binding site was 7.3 pmol/g brain, that of the .kappa.-binding site 6.7 pmol/g brain and that of the .delta.-binding site 2.0 pmol/g brain. The .kappa.-binding site had the lowest value whereas in the guinea-pig brain the capacity of the .mu.-binding site was lower than that of the .delta.- or .kappa.-binding site.

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