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- W2397828479 abstract "Previous studies have shown that central cholecystokinin (CCK) octapeptide (CCK-8) suppresses the binding of opioid receptors to the opioid agonists. In the present study, tritium-labelled etorphine (opioid agonist) and naloxone (opioid antagonist) as well as guanosine-5'-0-(3-thiotriphosphate) (GTPrS) were used to investigate the possible mechanisms underlying the suppression of opioid binding by CCK-8 in rat brain membranes. CCK-8 at a concentration range of 10 nmol/L to 1 mumol/L dose-dependently suppressed the binding of [3H]-naloxone to opioid receptors, with a decrease in Bmax and an increase in Kd. GTPrs was found to reduce the affinity of [3H]-etorphine binding in a dose-dependent manner. This effect was markedly diminished in the presence of 10 nmol/L of CCK-8. These results suggest that CCK-8 might suppress opioid binding at both the receptor and post-receptor levels; that is, 1) by reducing the number and affinity of opioid receptors, and 2) by uncoupling opioid receptors from their G proteins." @default.
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- W2397828479 date "1993-03-01" @default.
- W2397828479 modified "2023-09-26" @default.
- W2397828479 title "Modification of opioid receptors and uncoupling of receptors from G proteins as possible mechanisms underlying suppression of opioid binding by cholecystokinin octapeptide." @default.
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