Source:http://linkedlifedata.com/resource/pubmed/id/16563374
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1-2
|
| pubmed:dateCreated |
2006-4-17
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| pubmed:abstractText |
We previously demonstrated that dextromethorphan (DM; 3-methoxy-17-methylmorphinan) analogs have neuroprotective effects, and a recent report showed that DM reduces the adverse effects of morphine and blocks alpha3beta4 nicotinic acetylcholine receptors, a major target of anti-addictive agents. Here, we investigated the effects of DM, three of its analogs (DF, 3-methyl-17-methylmorphinan; AM, 3-allyloxy-17-methoxymorphian; and CM, 3-cyclopropyl-17-methoxymorphinan) and one of its metabolites (HM; 3-methoxymorphinan), on neuronal alpha3beta4 nicotinic acetylcholine receptor channel activity expressed in Xenopus laevis oocytes, using the two-microelectrode voltage clamp technique. We found that intraoocyte injection of neuronal alpha3 and beta4 nicotinic acetylcholine receptor subunit cRNAs elicited an inward current (IACh) in the presence of acetylcholine. Co-treatment with DM, DF, AM, CM or HM inhibited IACh in a dose-dependent, voltage-independent and reversible manner. The IC50 values for DM, DF, AM, CM and HM were 19.5+/-5.2, 15.8+/-4.5, 16.3+/-1.7, 10.1+/-2.8, and 13.5+/-4.0 microM, respectively. The order of potency for the inhibition of IACh was CM>HM>DF=AM>DM in oocytes expressing alpha3beta4 nicotinic acetylcholine receptors. The inhibitions of (IACh) by DM, DF and HM, AM and CM were non-competitive. These results indicate that AM, CM and HM could be novel non-competitive agents regulating alpha3beta4 nicotinic acetylcholine receptor channel activity.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
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| pubmed:month |
Apr
|
| pubmed:issn |
0014-2999
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| pubmed:author |
pubmed-author:ChoiSun-HyeSH,
pubmed-author:JeongSang MinSM,
pubmed-author:KimHyoung-ChunHC,
pubmed-author:KimJong-HoonJH,
pubmed-author:LeeByung-HwanBH,
pubmed-author:LeeJoon-HeeJH,
pubmed-author:LeeJun-HoJH,
pubmed-author:LeePhil HoPH,
pubmed-author:LeeSang-MokSM,
pubmed-author:NahSeung-YeolSY,
pubmed-author:ShinEun-JooEJ,
pubmed-author:YoonIn-SooIS
|
| pubmed:issnType |
Print
|
| pubmed:day |
24
|
| pubmed:volume |
536
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
85-92
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| pubmed:dateRevised |
2006-11-15
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| pubmed:meshHeading |
pubmed-meshheading:16563374-Animals,
pubmed-meshheading:16563374-Cattle,
pubmed-meshheading:16563374-Dextromethorphan,
pubmed-meshheading:16563374-Dose-Response Relationship, Drug,
pubmed-meshheading:16563374-Electric Stimulation,
pubmed-meshheading:16563374-Female,
pubmed-meshheading:16563374-Gene Expression,
pubmed-meshheading:16563374-Membrane Potentials,
pubmed-meshheading:16563374-Molecular Structure,
pubmed-meshheading:16563374-Oocytes,
pubmed-meshheading:16563374-RNA, Complementary,
pubmed-meshheading:16563374-Receptors, Nicotinic,
pubmed-meshheading:16563374-Structure-Activity Relationship,
pubmed-meshheading:16563374-Time Factors,
pubmed-meshheading:16563374-Xenopus laevis
|
| pubmed:year |
2006
|
| pubmed:articleTitle |
Effects of dextrorotatory morphinans on alpha3beta4 nicotinic acetylcholine receptors expressed in Xenopus oocytes.
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| pubmed:affiliation |
Department of Physiology, College of Veterinary Medicine, Konkuk University, Institute of Biomedical Science and Technology, and Bio/Molecular Informatics Center, Seoul, Republic of Korea.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|