Abstract

Regulation by guanine nucleotides (G) and cations of ligand binding to frog (Rana esculenta) brain opioid receptors was investigated in the present study. The binding of the benzomorphan opioid [ 3 H]ethylketocyclazocine, (EKC) displayed either agonist- or antagonist-type behaviour depending upon the assay temperature. Thus, [ 3 H]EKC binding was increased by G and Na + at 4 o C, whereas it was inhibited by Mg 2+ . In contrast, G and Na + decreased the specific ligand binding at 33 o C. Our data suggest that the temperature dependence of opioid receptor-G protein coupling might be of great importance in frog brain

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