Review ArticleReview Article
Regulation of µ-Opioid Receptors: Desensitization, Phosphorylation, Internalization, and Tolerance
John T. Williams, Susan L. Ingram, Graeme Henderson, Charles Chavkin, Mark von Zastrow, Stefan Schulz, Thomas Koch, Christopher J. Evans and MacDonald J. Christie
Annette C. Dolphin, ASSOCIATE EDITOR, Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Pharmacological Reviews January 2013, 65 (1) 223-254; DOI: https://doi.org/10.1124/pr.112.005942
John T. Williams
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Susan L. Ingram
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Graeme Henderson
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Charles Chavkin
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Mark von Zastrow
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Stefan Schulz
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Thomas Koch
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Christopher J. Evans
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
MacDonald J. Christie
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
Annette C. Dolphin
Vollum Institute, Oregon Health Sciences University, Portland, Oregon (J.T.W.); Department of Neurologic Surgery, Oregon Health Sciences University, Portland, Oregon (S.L.I.); School of Physiology and Pharmacology, University of Bristol, Bristol, United Kingdom (G.H.); Department of Pharmacology, University of Washington, Seattle, Washington (C.C.); Psychiatry and Pharmacology, University of California at San Francisco, San Francisco, California (M.v.Z.); Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany (S.S.); Institute of Pharmacology and Toxicology, University of Magdeburg, Magdeburg, Germany (T.K.); Hatos Center of Neuropharmacology, University of California at Los Angeles (C.J.E.); and Discipline of Pharmacology, University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
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In this issue
Review ArticleReview Article
Regulation of μ-Opioid Receptors
John T. Williams, Susan L. Ingram, Graeme Henderson, Charles Chavkin, Mark von Zastrow, Stefan Schulz, Thomas Koch, Christopher J. Evans and MacDonald J. Christie
Pharmacological Reviews January 1, 2013, 65 (1) 223-254; DOI: https://doi.org/10.1124/pr.112.005942
Review ArticleReview Article
Regulation of μ-Opioid Receptors
John T. Williams, Susan L. Ingram, Graeme Henderson, Charles Chavkin, Mark von Zastrow, Stefan Schulz, Thomas Koch, Christopher J. Evans and MacDonald J. Christie
Pharmacological Reviews January 1, 2013, 65 (1) 223-254; DOI: https://doi.org/10.1124/pr.112.005942
Jump to section
- Article
- Abstract
- I. Introduction
- II. Definition of Terms
- III. Structure and Function of μ-Opioid Receptors
- IV. μ-Opioid Receptor Regulation
- V. Phosphorylation and μ-Opioid Receptor Regulation
- VI. Internalization, Phosphatase Activity, and Recovery from Desensitization
- VII. Cellular Adaptations Induced during Morphine Tolerance
- VIII. Implications and Outstanding Questions
- IX. Concluding Remarks
- Acknowledgments
- Authorship Contibutions
- Footnotes
- Abbreviations
- REFERENCES
- Figures & Data
- Info & Metrics
- eLetters
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