Source:http://linkedlifedata.com/resource/pubmed/id/10688980
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2-3
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pubmed:dateCreated |
2000-4-18
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pubmed:abstractText |
Human neuroblastoma SH-SY5Y cells express endogenous mu-opioid receptor and develop cellular tolerance to morphine after prolonged (>/=4 h) treatment with morphine. Treatment with forskolin (25 microM, 12 h), an adenylyl cyclase activator, also desensitized mu-opioid receptor response to morphine (10 microM) by 38% (P<0. 001), which was reversed by the cyclic AMP (cAMP) dependent kinase inhibitor N-(2-aminoethyl)-5-isoquinolinesulfonamide (H8) (100 microM). Treatment with both morphine and forskolin appeared to cause an additive effect in desensitizing mu-opioid receptor. In mu-opioid receptor stably transfected human embryonic kidney 293 (HEK-mu) cells, morphine treatment produced cAMP upregulation, yet failed to induce mu-opioid receptor tolerance. However, treatment with forskolin (25 microM) or 8-bromo-cAMP (1mM) led to profound mu-opioid receptor tolerance, which was reversed by H8. These results demonstrate that cAMP-dependent kinase activation causes mu-opioid receptor tolerance. However, morphine-induced mu-opioid receptor tolerance in SH-SY5Y cells is not mediated by cAMP-dependent kinase activation. In addition, our results indicate that cAMP-upregulation does not necessarily lead to mu-opioid receptor tolerance.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP-Dependent Protein Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Forskolin,
http://linkedlifedata.com/resource/pubmed/chemical/Morphine,
http://linkedlifedata.com/resource/pubmed/chemical/Narcotics,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
18
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pubmed:volume |
389
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
165-71
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:10688980-Cyclic AMP,
pubmed-meshheading:10688980-Cyclic AMP-Dependent Protein Kinases,
pubmed-meshheading:10688980-Drug Tolerance,
pubmed-meshheading:10688980-Enzyme Activation,
pubmed-meshheading:10688980-Forskolin,
pubmed-meshheading:10688980-Humans,
pubmed-meshheading:10688980-Morphine,
pubmed-meshheading:10688980-Narcotics,
pubmed-meshheading:10688980-Phosphorylation,
pubmed-meshheading:10688980-Receptors, Opioid, mu,
pubmed-meshheading:10688980-Tumor Cells, Cultured
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pubmed:year |
2000
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pubmed:articleTitle |
Tolerance to morphine at the mu-opioid receptor differentially induced by cAMP-dependent protein kinase activation and morphine.
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pubmed:affiliation |
Department of Pharmaceutical Chemistry, University of California, San Francisco, CA, USA. zwang@u.arizona.edu
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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