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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2008-2-5
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pubmed:abstractText |
From hit compounds identified by high throughput screening (HTS), we have found compound 1 as a lead TRPV1 antagonist and confirmed its potential as a treatment for pain. Compound 1 has led to potent TRPV1 antagonistic benzamide derivatives ((+/-)-2: human IC(50)=23 nM, (+/-)-3: human IC(50)=14 nM in the capsaicin-induced calcium influx assay) containing indole and naphthyl moieties, obtained by elaboration of the tryptamine scaffold or via bioisosteric replacements.
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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 |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:IkedaTakafumiT,
pubmed-author:Iki-TakiAyakoA,
pubmed-author:ItoFumitakaF,
pubmed-author:JinnoMadokaM,
pubmed-author:KanaiYoshihitoY,
pubmed-author:MakitaNaoyaN,
pubmed-author:OhmiTakashiT,
pubmed-author:OhtaAtsukoA,
pubmed-author:ShimojoMasatoM,
pubmed-author:ShishidoYujiY,
pubmed-author:SudoMasakiM,
pubmed-author:TamuraTetsuyaT
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pubmed:issnType |
Electronic
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pubmed:day |
1
|
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pubmed:volume |
18
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pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
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pubmed:pagination |
1072-8
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pubmed:meshHeading |
|
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis of benzamide derivatives as TRPV1 antagonists.
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pubmed:affiliation |
Pfizer Global Research & Development, Nagoya Laboratories, 5-2 Taketoyo, Aichi 470-2394, Japan. Yuji.Shishido@pfizer.com
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pubmed:publicationType |
Journal Article
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