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Cited by 159

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Differential regulation by cAMP-dependent protein kinase and protein kinase C of the mu opioid receptor coupling to a G protein-activated K+ channel.

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Chen, Y., Yu, L.·1994·Journal of Biological Chemistry

Abstract

A mu opioid receptor and a G protein-activated K+ channel were coexpressed in Xenopus oocytes. Stimulation of the mu opioid receptor induced an inwardly rectifying current that was blocked by opioid receptor antagonist naloxone, indicating that the mu opioid receptor is functionally coupled to the K+ channel. The coupling is mediated by G proteins, since pertussis toxin treatment reduced the K+ current and injection of GTP gamma S (guanosine 5'-O-(thiotriphosphate)) enhanced it. Repeated stimulation of the mu receptor leads to desensitization, as the K+ current from the second stimulation was reduced to 70% of that from the first one. Both cAMP-dependent protein kinase (PKA) and protein kinase C (PKC) regulate this process, but in opposite direction. Activation of PKC by treatment of the oocyte with phorbol ester potentiated the desensitization of the mu receptor-induced current. However, incubation of the cell with a membrane-permeable cAMP analog, 8-chlorophenylthio-cAMP, completely abolished the desensitization. The cAMP effect appears to be mediated by PKA, since injection of a PKA catalytic subunit showed the same effect as cAMP incubation. These results suggest that PKA and PKC differentially regulate the mu opioid receptor coupling to the G protein-activated K+ channel.

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Metadata

Authors
Chen, Y., & Yu, L.
Venue
Journal of Biological Chemistry
Publisher
Elsevier BV
Published
1994-03
Volume
269
Issue
11
Pages
7839-7842
ISSN
0021-9258 (ISSN-L)
OpenAlex
W1573285735
Cited by
159
References
0
FWCI
6.74
Type
journal article
Language
en
Open access
hybrid

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CoChat. (2026). Citation check: Differential regulation by cAMP-dependent protein kinase and protein kinase C of the mu opioid receptor coupling to a G protein-activated K+ channel. https://app.cochat.ai/papers/10.1016/s0021-9258(17)37124-7
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Chen, Y., & Yu, L. (1994). Differential regulation by cAMP-dependent protein kinase and protein kinase C of the mu opioid receptor coupling to a G protein-activated K+ channel. Journal of Biological Chemistry. https://doi.org/10.1016/s0021-9258(17)37124-7

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