Abstract
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.
Publication types
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Comparative Study
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amino Acid Substitution
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Animals
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CHO Cells
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Cricetinae
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Cricetulus
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Humans
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Morphine / pharmacology*
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Mutation
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Oligopeptides / pharmacology
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Phosphorylation / drug effects
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Receptors, Opioid, delta / agonists
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Receptors, Opioid, delta / genetics
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Receptors, Opioid, delta / metabolism*
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Serine / genetics
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Serine / metabolism
Substances
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Oligopeptides
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Receptors, Opioid, delta
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deltorphin II, Ala(2)-
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Serine
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Morphine