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rdf:type |
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lifeskim:mentions |
umls-concept:C0020792,
umls-concept:C0026336,
umls-concept:C0026339,
umls-concept:C0150055,
umls-concept:C0205314,
umls-concept:C0205460,
umls-concept:C0243076,
umls-concept:C0679622,
umls-concept:C1421467,
umls-concept:C1704419,
umls-concept:C1880022
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pubmed:issue |
2
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pubmed:dateCreated |
2006-1-19
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pubmed:abstractText |
Vanilloid receptor 1 (VR1, TRPV1) is a cation-selective ion channel that is expressed on primary afferent neurons and is upregulated following inflammation and nerve damage. Blockers of this channel may have utility in the treatment of chronic nociceptive and neuropathic pain. Here, we describe the optimization from a high throughput screening hit, of a series of 6-aryl-7-isopropylquinazolinones that are TRPV1 antagonists in vitro. We also demonstrate that one compound is active in vivo against capsaicin-induced hyperalgesia and in models of neuropathic and nociceptive pain in the rat.
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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 |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BevanStuartS,
pubmed-author:ChristiansenMartinM,
pubmed-author:CoppPrafulaP,
pubmed-author:CulshawAndrew JAJ,
pubmed-author:DavisAndrewA,
pubmed-author:DavisClareC,
pubmed-author:DysonAlexA,
pubmed-author:DziadulewiczEdward KEK,
pubmed-author:EdwardsLeeL,
pubmed-author:EggelteHendrikusH,
pubmed-author:FoxAlysonA,
pubmed-author:GentryCliveC,
pubmed-author:GroarkeAlexA,
pubmed-author:HallettAllanA,
pubmed-author:HartTerance WTW,
pubmed-author:HughesGlyn AGA,
pubmed-author:KnightsSallyS,
pubmed-author:KotsonisPeterP,
pubmed-author:LyothierIsabelleI,
pubmed-author:McBrydeAndrewA,
pubmed-author:McIntyrePeterP,
pubmed-author:PaloumbisGeorgeG,
pubmed-author:PanesarMohM,
pubmed-author:PatelSadhanaS,
pubmed-author:SeilerMax-PeterMP,
pubmed-author:WinN ANA,
pubmed-author:YaqoobMohammedM,
pubmed-author:ZimmermannKasparK
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pubmed:issnType |
Print
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pubmed:day |
26
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
471-4
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16420034-Animals,
pubmed-meshheading:16420034-Blood-Brain Barrier,
pubmed-meshheading:16420034-CHO Cells,
pubmed-meshheading:16420034-Caco-2 Cells,
pubmed-meshheading:16420034-Cell Membrane Permeability,
pubmed-meshheading:16420034-Chronic Disease,
pubmed-meshheading:16420034-Cricetinae,
pubmed-meshheading:16420034-Cricetulus,
pubmed-meshheading:16420034-Disease Models, Animal,
pubmed-meshheading:16420034-Humans,
pubmed-meshheading:16420034-Mice,
pubmed-meshheading:16420034-Micronucleus Tests,
pubmed-meshheading:16420034-Microsomes, Liver,
pubmed-meshheading:16420034-Pain,
pubmed-meshheading:16420034-Quinazolines,
pubmed-meshheading:16420034-Rats,
pubmed-meshheading:16420034-Solubility,
pubmed-meshheading:16420034-Structure-Activity Relationship,
pubmed-meshheading:16420034-TRPV Cation Channels
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pubmed:year |
2006
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pubmed:articleTitle |
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
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pubmed:affiliation |
Novartis Institutes for Biomedical Research, London WC1E 6BS, UK. andrew.culshaw@novartis.com
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pubmed:publicationType |
Journal Article,
In Vitro
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