Morphine promotes phosphorylation of the human delta-opioid receptor at serine 363.
After prolonged stimulation, the delta-opioid receptor becomes desensitized by regulatory mechanisms such as receptor phosphorylation, internalization and down-regulation. In this study, we demonstrate that morphine treatment causes phosphorylation of S363 in the C-terminus of the human delta-opioid receptor. Morphine-mediated phosphorylation reached 53+/-8% of maximum deltorphin II-mediated phosphorylation. Phosphorylation of S363 may contribute to delta-opioid receptor desensitization by morphine.
Navratilova
Edita
E
Department of Medical Pharmacology, College of Medicine, The University of Arizona, Tucson, AZ 85724, USA.
Eaton
Miriam C
MC
Stropova
Dagmar
D
Varga
Eva V
EV
Vanderah
Todd W
TW
Roeske
William R
WR
Yamamura
Henry I
HI
D019943:Amino Acid Substitution; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D009020:Morphine / Q000494:pharmacology*; D009154:Mutation; D009842:Oligopeptides / Q000494:pharmacology; D010766:Phosphorylation / Q000187:drug effects; D017465:Receptors, Opioid, delta / Q000819:agonists / Q000235:genetics / Q000378:metabolism*; D012694:Serine / Q000235:genetics / Q000378:metabolism
D009842:Oligopeptides; D017465:Receptors, Opioid, delta; C060209:deltorphin II, Ala(2)-; D012694:Serine; D009020:Morphine