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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2010-10-19
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pubmed:abstractText |
A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1) provided potent, selective derivatives with improved aqueous solubility and oral bioavailability. Representative compounds from this series displayed efficacy in rat models of inflammatory and neuropathic pain.
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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 |
Nov
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AntonioBrettB,
pubmed-author:AtkinsonRobert NRN,
pubmed-author:ChapmanMark LML,
pubmed-author:DrizinIreneI,
pubmed-author:FaltynekConnie RCR,
pubmed-author:GreggRobert JRJ,
pubmed-author:HakeemAhmed HAH,
pubmed-author:HonorePriscaP,
pubmed-author:JarvisMichael FMF,
pubmed-author:JohnsonMatthew SMS,
pubmed-author:JoshiShailenS,
pubmed-author:KortMichael EME,
pubmed-author:KrafteDouglas SDS,
pubmed-author:KrambisMichael JMJ,
pubmed-author:LiuDongD,
pubmed-author:MarronBrian EBE,
pubmed-author:MarshKennan CKC,
pubmed-author:MatulenkoMark AMA,
pubmed-author:MikusaJoseph PJP,
pubmed-author:RoeloffsRosemarieR,
pubmed-author:ScanioMarc J CMJ,
pubmed-author:SecrestMatthew AMA,
pubmed-author:ShiLeiL,
pubmed-author:ShiehChar-ChangCC,
pubmed-author:SimlerGriceldaG,
pubmed-author:ThomasJames BJB,
pubmed-author:WernessStephenS,
pubmed-author:ZhangXuFengX,
pubmed-author:ZhongChengminC
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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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 |
6812-5
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pubmed:meshHeading |
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pubmed:year |
2010
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pubmed:articleTitle |
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
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pubmed:affiliation |
Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA. michael.e.kort@abbott.com
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pubmed:publicationType |
Journal Article
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