Source:http://linkedlifedata.com/resource/pubmed/id/16258243
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2005-10-31
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pubmed:abstractText |
The flavonoid, quercetin, is a low molecular weight substance found in apple, tomato and other fruit. Besides its antioxidative effect, quercetin, like other flavonoids, has a wide range of neuropharmacological actions including analgesia, and motility, sleep, anticonvulsant, sedative and anxiolytic effects. In the present study, we investigated its effect on mouse 5-hydroxytryptamine type 3 (5-HT3A) receptor channel activity, which is involved in pain transmission, analgesia, vomiting, and mood disorders. The 5-HT3A receptor was expressed in Xenopus oocytes, and the current was measured with the two-electrode voltage clamp technique. In oocytes injected with 5-HT3A receptor cRNA, quercetin inhibited the 5-HT-induced inward peak current (I(5-HT)) with an IC50 of 64.7 +/- 2.2 microM. Inhibition was competitive and voltage-independent. Point mutations of pre-transmembrane domain 1 (pre-TM1) such as R222T and R222A, but not R222D, R222E and R222K, abolished inhibition, indicating that quercetin interacts with the pre-TM1 of the 5-HT3A receptor.
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pubmed:commentsCorrections | |
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 |
Aug
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pubmed:issn |
1016-8478
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pubmed:author |
pubmed-author:ChangChoon-GonCG,
pubmed-author:ChoiSun-HyeSH,
pubmed-author:HanYeSunY,
pubmed-author:JeongSang-MinSM,
pubmed-author:JungSang-MinSM,
pubmed-author:KimHyung-ChunHC,
pubmed-author:KimJong-HoonJH,
pubmed-author:KimYangmeeY,
pubmed-author:LeeByung-HwanBH,
pubmed-author:LeeJoon-HeeJH,
pubmed-author:LeeJun-HoJH,
pubmed-author:LeeSang-MokSM,
pubmed-author:NahSeung-YeolSY,
pubmed-author:PaikHyun-DongHD,
pubmed-author:YoonIn-SooIS
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pubmed:issnType |
Print
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pubmed:day |
31
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
69-73
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:16258243-Animals,
pubmed-meshheading:16258243-Dose-Response Relationship, Drug,
pubmed-meshheading:16258243-Female,
pubmed-meshheading:16258243-Ion Channel Gating,
pubmed-meshheading:16258243-Ion Transport,
pubmed-meshheading:16258243-Membrane Potentials,
pubmed-meshheading:16258243-Mice,
pubmed-meshheading:16258243-Mutagenesis, Site-Directed,
pubmed-meshheading:16258243-Oocytes,
pubmed-meshheading:16258243-Protein Structure, Tertiary,
pubmed-meshheading:16258243-Quercetin,
pubmed-meshheading:16258243-Receptors, Serotonin, 5-HT3,
pubmed-meshheading:16258243-Serotonin 5-HT3 Receptor Antagonists,
pubmed-meshheading:16258243-Xenopus laevis
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pubmed:year |
2005
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pubmed:articleTitle |
Quercetin inhibits the 5-hydroxytryptamine type 3 receptor-mediated ion current by interacting with pre-transmembrane domain I.
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pubmed:affiliation |
Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University, Seoul 143-701, Korea.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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