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- W2392111310 abstract "Objective:To investigate the effects of agmatine by activation of I1 imidazoline receptor on DAMGO [(D-Ala2,N-Me-Phe4,Gly5-ol)-enkephalin]-induced desensitization and down-regulation of μ-opioid receptor.Methods: Two cell lines,Chinese hamster ovary cells expressing μ-opioid receptor alone(CHO-μ) and co-expressing μ-opioid receptor and imidazoline receptor antisera-selected protein(IRAS),CHO-μ/IRAS i.e.a candidate for I1 imidazoline receptor,were used.GTPγS binding assay and diprenorphine binding assay were used to determine the effect on the desensitization and down-regulation of μ-opioid receptor by the agmatine-I1 imidazoline receptor system.Results: There was no significant difference in expression and affinity of μ-opioid receptor between normal CHO-μ and CHO-μ/IRAS cells.The reaction of μ-opioid receptor in both cells was equal to the stimulation of ligand.DAMGO 10 μmol/L treatment for 30 min induced desensitization of μ-opioid receptor in CHO-μ/IRAS cells,while agmatine(10 nmol/L-10 μmol/L)did not influence DAMGO-induced desensitization of μ-opioid receptor.Chronic treatment with DAMGO(1 μmol/L,12 h) decreased the expression of μ-opioid receptor in CHO-μ and CHO-μ/IRAS cells.Agmatine(1-100 nM) concentration-dependently inhibited DAMGO-induced down-regulation of μ-opioid receptor in CHO-μ/IRAS cells,while this effect was not observed in CHO-μ cells.Efaroxan,an I1 imidazoline receptor-preferential antagonist,completely reversed the effect of agmatine in CHO-μ/IRAS cell.Conclusion: Agmatine could inhibit DAMGO-induced down-regulation of μ-opioid receptor by activation of I1 imidazoline receptor,which may contribute to the inhibition of opioid dependence by agmatine." @default.
- W2392111310 created "2016-06-24" @default.
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- W2392111310 date "2007-01-01" @default.
- W2392111310 modified "2023-09-25" @default.
- W2392111310 title "Modulating effect of agmatine on desensitization and down-regulation of μ-opioid receptor by activation of I1 imidazoline receptor" @default.
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