PMID: 9526035Apr 4, 1998Paper

Role of carboxyl terminus of mu-and delta-opioid receptor in agonist-induced down-regulation

Brain Research. Molecular Brain Research
E A AfifyH H Loh

Abstract

Chronic exposure of mu-and delta-opioid receptors to their agonists leads to different rates in receptor down-regulation. In order to analyze the role of the carboxyl terminus of mu-and delta-opioid receptors in the difference in the rate of down-regulation, two chimeras of these receptors were generated by swapping the carboxyl termini; MORTAGDT and DORTAGMT. These chimeras were tagged at the N-terminus with hemagglutinin (HA) epitope (YPYDVPDYA), which can be recognized by the monoclonal antibody 12CA5, and then stably expressed in Neuro 2A (N2A) cells. The swapping of the carboxyl termini did not alter the ligand selectivity of these receptor chimeras. However, they did exhibit a reduction in agonist potency to inhibit forskolin-stimulated adenylyl cyclase activity for all agonists tested except etorphine which had a potency comparable to that of wild type receptors. Treatment of the N2A cells expressing MORTAGDT with 50 nM etorphine produced a faster rate of receptor down-regulation when compared to the wild type mu-opioid receptor. Immunofluorescence microscopy of the MORTAGDT chimera using a monoclonal antibody against HA confirmed internalization of the receptors after treatment with etorphine for 1 and 6h. There was a r...Continue Reading

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Citations

Nov 11, 2003·Life Sciences·Hiroshi UedaKiyonobu Mizuno
Nov 8, 2001·European Journal of Pharmacology·Z Wiesenfeld-Hallin, X J Xu
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May 7, 2021·Movement Disorders : Official Journal of the Movement Disorder Society·Valtteri KaasinenAngelo Antonini

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