Wang et al., Neuropharmacology 2000
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To investigate the functional role of G protein coupled receptor kinases ( GRK ) in homologous desensitization of the mu-opioid receptor , human embryonic kidney (HEK) 293 cells, which express a significant level of GRK2, were stably transfected with the cDNA encoding the rat mu-opioid receptor
Bailey et al., Mol Pharmacol 2004
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This is the first finding that morphine can induce rapid mu-opioid receptor desensitization in adult rat neurons, and because reduced protein kinase C activity in vivo attenuates morphine tolerance, we propose that G-protein coupled receptor cross-talk and the level of protein kinase C activity may play critical roles in the desensitization of the mu-opioid receptor and could underlie the development of morphine tolerance