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Research ArticleArticle

Role of mPKCI, a Novel μ-Opioid Receptor Interactive Protein, in Receptor Desensitization, Phosphorylation, and Morphine-Induced Analgesia

Wei Guang, Hongyan Wang, Tao Su, I. Bernard Weinstein and Jia Bei Wang
Molecular Pharmacology November 2004, 66 (5) 1285-1292; DOI: https://doi.org/10.1124/mol.66.5.1285
Wei Guang
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Hongyan Wang
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Tao Su
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I. Bernard Weinstein
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Jia Bei Wang
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Abstract

The human μ-opioid receptor (HμOR) is a G-protein coupled receptor that mediates analgesia, euphoria and other important central and peripheral neurological functions. In this study, we found in a yeast two-hybrid screen that a protein kinase C-interacting protein (PKCI) specifically interacts with the C terminus of HμOR. The interaction of PKCI with HμOR was recapitulated in Chinese hamster ovary cells that express the full-length HμOR and PKCI proteins. The affinity of HμOR for an opioid ligand and its ability to mediate the activation of a G-protein were not altered by their interaction. However, the association of PKCI with HμOR reduced agonist-induced inhibition of adenylyl cyclase and suppressed HμOR desensitization partially at the G protein level and completely at the adenylyl cyclase level. Furthermore, PMA-induced, but not DAMGO-induced, HμOR phosphorylation was partially inhibited by the coexpression of PKCI, suggesting that PKCI exerts a selective regulatory effect on HμOR signaling. This effect was specific to the μ-opioid receptor because δ-opioid receptor desensitization was unaffected by PKCI. In addition, behavioral studies revealed that both basal and morphine-induced analgesia were significantly enhanced in the mutant mice that lacked expression of PKCI gene, and these mice developed a greater extent of tolerance to morphine analgesia. Taken together, these results suggest that PKCI functions as a negative regulator in HμOR desensitization, phosphorylation, and in mediating morphine analgesia.

  • Received February 25, 2004.
  • Accepted July 27, 2004.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 66 (5)
Molecular Pharmacology
Vol. 66, Issue 5
1 Nov 2004
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Research ArticleArticle

Role of mPKCI, a Novel μ-Opioid Receptor Interactive Protein, in Receptor Desensitization, Phosphorylation, and Morphine-Induced Analgesia

Wei Guang, Hongyan Wang, Tao Su, I. Bernard Weinstein and Jia Bei Wang
Molecular Pharmacology November 1, 2004, 66 (5) 1285-1292; DOI: https://doi.org/10.1124/mol.66.5.1285

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Research ArticleArticle

Role of mPKCI, a Novel μ-Opioid Receptor Interactive Protein, in Receptor Desensitization, Phosphorylation, and Morphine-Induced Analgesia

Wei Guang, Hongyan Wang, Tao Su, I. Bernard Weinstein and Jia Bei Wang
Molecular Pharmacology November 1, 2004, 66 (5) 1285-1292; DOI: https://doi.org/10.1124/mol.66.5.1285
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