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- W2414606987 abstract "Monovalent cations such as Na+, K+ and Li+ at 100 mM concentration inhibit the binding of mu and delta opioid agonists (e.g. (3H) dihydromorphine and (3H) D-Ala2-Leu5-enkephalin), enhance opioid antagonist [(3H) naloxone] binding in rat brain membranes. Divalent cations have an opposite effect: Mg2+ or Mn2+ (2mM) increase both mu and delta agonist binding, and decrease the antagonist binding. The effect of guanosine 5'-triphosphate and its non-hydrolysable analogue 5'-guanylyl-imidodiphosphate at micromolar concentrations is similar to that of sodium ion. In kinetic experiments, guanine nucleotides promote the dissociation of radiolabelled agonists from their binding sites by increasing the rate of dissociation. Equilibrium saturation binding studies show that only binding of the opioid agonist ligands are significantly inhibited by 5'-guanylyl-imidodiphosphate." @default.
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- W2414606987 date "1989-01-01" @default.
- W2414606987 modified "2023-10-17" @default.
- W2414606987 title "Cation and guanine nucleotide effects on ligand binding properties of mu and delta opioid receptors in rat brain membranes." @default.
- W2414606987 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2558475" @default.
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