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- W2084844186 abstract "This study shows that nucleotides, as well as ions, regulate the opiate receptors of brain. GMP-P(NH)P and Na + reduce the amount of steady-state specific [ 3 H]dihydromorphine binding and increase the rate of dissociation of the ligand from the opiate receptor. In contrast, Mn 2+ decreases the rate of ligand dissociation and antagonizes the ability of Na + to increase dissociation. The effects of GMP-P(NH)P on steady-state binding and dissociation are not reversed by washing. Only GTP, GDP, ITP, and IMP-P(NH)P, in addition to GMP-P(NH)P, increase the rate of dihydromorphine dissociation. The site of nucleotide action appears to have high affinity: <1 μM GMP-P(NH)P produces half-maximal increases in ligand dissociation. GMP-P(NH)P- and Na + -directed increases in dissociation have also been found for the opiate agonists [ 3 H]etorphine, [ 3 H]Leu-enkephalin, and [ 3 H]Met-enkephalin and the opiate antagonist [ 3 H]naltrexone. Mn 2+ -directed decreases in dissociation have been found for the agonist [ 3 H]-etorphine and the antagonist [ 3 H]naltrexone. Although the plasma membrane receptors for a number of other neuro-transmitters and hormones are also regulated by guanine nucleotides, the opiate receptors appear unique because only they show nucleotide regulation of both agonist and antagonist binding." @default.
- W2084844186 created "2016-06-24" @default.
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- W2084844186 date "1978-04-01" @default.
- W2084844186 modified "2023-10-18" @default.
- W2084844186 title "Interaction of ligands with the opiate receptors of brain membranes: Regulation by ions and nucleotides" @default.
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- W2084844186 doi "https://doi.org/10.1073/pnas.75.4.1713" @default.
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