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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2004-6-18
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pubmed:abstractText |
Small molecule antagonists of the vanilloid receptor 1 (TRPV1, also known as VR1) are disclosed. Ureas such as 5 (SB-452533) were used to explore the structure activity relationship with several potent analogues identified. Pharmacological studies using electrophysiological and FLIPR Ca(2+) based assays showed compound 5 was an antagonist versus capsaicin, noxious heat and acid mediated activation of TRPV1. Study of a quaternary salt of 5 supports a mode of action in which compounds from this series cause inhibition via an extracellularly accessible binding site on the TRPV1 receptor.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BroughStephenS,
pubmed-author:DavisJohn BJB,
pubmed-author:EgertonJulieJ,
pubmed-author:GunthorpeMartin JMJ,
pubmed-author:JermanJeffrey CJC,
pubmed-author:RamiHarshad KHK,
pubmed-author:RandallAndrew DAD,
pubmed-author:SmartDarrenD,
pubmed-author:StevensAlexander JAJ,
pubmed-author:ThompsonMervynM,
pubmed-author:WymanPaulP
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pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3631-4
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:15203132-Aminobiphenyl Compounds,
pubmed-meshheading:15203132-Animals,
pubmed-meshheading:15203132-Binding Sites,
pubmed-meshheading:15203132-Calcium,
pubmed-meshheading:15203132-Capsaicin,
pubmed-meshheading:15203132-Cell Line,
pubmed-meshheading:15203132-Electrophysiology,
pubmed-meshheading:15203132-Fluorescence,
pubmed-meshheading:15203132-Hot Temperature,
pubmed-meshheading:15203132-Humans,
pubmed-meshheading:15203132-Hydrogen-Ion Concentration,
pubmed-meshheading:15203132-Image Enhancement,
pubmed-meshheading:15203132-Patch-Clamp Techniques,
pubmed-meshheading:15203132-Rats,
pubmed-meshheading:15203132-Receptors, Drug,
pubmed-meshheading:15203132-Structure-Activity Relationship,
pubmed-meshheading:15203132-TRPV Cation Channels
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pubmed:year |
2004
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pubmed:articleTitle |
Discovery of small molecule antagonists of TRPV1.
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pubmed:affiliation |
Neurology and GI CEDD, New Frontiers Science Park, GlaxoSmithKline, Third Avenue, Harlow, Essex CM19 5AW, UK. harshad.rami@gsk.com
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pubmed:publicationType |
Journal Article
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