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Protein kinase C involvement in homologous desensitization of delta- opioid receptor coupled to Gi1-phospholipase C activation in Xenopus oocytes

H Ueda, T Miyamae, C Hayashi, S Watanabe, N Fukushima, Y Sasaki, T Iwamura and Y Misu
Journal of Neuroscience 1 November 1995, 15 (11) 7485-7499; DOI: https://doi.org/10.1523/JNEUROSCI.15-11-07485.1995
H Ueda
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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T Miyamae
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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C Hayashi
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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S Watanabe
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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N Fukushima
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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Y Sasaki
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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T Iwamura
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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Y Misu
Department of Pharmacology, Yokohama City University School of Medicine, Japan.
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Abstract

We have developed the coexpression system of both delta-opioid receptor (DOR1) and M2-muscarinic receptor (M2) which mediate agonist-evoked currents due to common post-receptor mechanisms including Gi1 and phospholipase C (PLC) activation in Xenopus oocytes reconstituted with Gi1 alpha. The DOR1-currents by 100 nM D-Ser2-leu-enkephalin-Thr6 (DSLET) were selectively desensitized by 10 nM phorbol 12-myristate 13- acetate (PMA). The PMA-desensitization of DSLET-currents was abolished in the presence of calphostin C, a protein kinase C inhibitor, or reversed by an intracellular injection of calcineurin, a protein phosphatase 2B. When a higher concentration (3 microM) of DSLET was used, DSLET-currents were rapidly desensitized by repeated challenges of DSLET itself. However, repeated challenges of 10 microM ACh caused no influence on such DSLET- or M2-currents. The desensitization of DSLET-currents was selectively reversed by protein kinase C inhibitors. Similar results were also obtained with various delta-opioid agonists. These results suggest that protein kinase Cis involved in the homologous desensitization of delta-opioid receptors.

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The Journal of Neuroscience: 15 (11)
Journal of Neuroscience
Vol. 15, Issue 11
1 Nov 1995
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Protein kinase C involvement in homologous desensitization of delta- opioid receptor coupled to Gi1-phospholipase C activation in Xenopus oocytes
H Ueda, T Miyamae, C Hayashi, S Watanabe, N Fukushima, Y Sasaki, T Iwamura, Y Misu
Journal of Neuroscience 1 November 1995, 15 (11) 7485-7499; DOI: 10.1523/JNEUROSCI.15-11-07485.1995

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Protein kinase C involvement in homologous desensitization of delta- opioid receptor coupled to Gi1-phospholipase C activation in Xenopus oocytes
H Ueda, T Miyamae, C Hayashi, S Watanabe, N Fukushima, Y Sasaki, T Iwamura, Y Misu
Journal of Neuroscience 1 November 1995, 15 (11) 7485-7499; DOI: 10.1523/JNEUROSCI.15-11-07485.1995
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