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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2010-8-16
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pubmed:abstractText |
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was identified as a potent P2X(7) antagonist with excellent in vivo activity in animal models of pain, and a profile suitable for progression to clinical studies.
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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 |
Sep
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AbdiMuna HMH,
pubmed-author:BeswickPaul JPJ,
pubmed-author:BillintonAndyA,
pubmed-author:ChambersLaura JLJ,
pubmed-author:CharltonAndrewA,
pubmed-author:CollinsSue DSD,
pubmed-author:CollisKatharine LKL,
pubmed-author:DeanDavid KDK,
pubmed-author:FonfriaElenaE,
pubmed-author:GleaveRobert JRJ,
pubmed-author:LejeuneClarisse LCL,
pubmed-author:LivermoreDavid GDG,
pubmed-author:MedhurstStephen JSJ,
pubmed-author:MichelAnton DAD,
pubmed-author:MosesAndrew PAP,
pubmed-author:PageLeeL,
pubmed-author:PatelSadhanaS,
pubmed-author:RomanShilina ASA,
pubmed-author:SengerStefanS,
pubmed-author:SlingsbyBrianB,
pubmed-author:SteadmanJon G AJG,
pubmed-author:StevensAlexander JAJ,
pubmed-author:WalterDaryl SDS
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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 |
1
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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 |
5080-4
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pubmed:meshHeading |
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pubmed:year |
2010
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pubmed:articleTitle |
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
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pubmed:affiliation |
Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK.
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pubmed:publicationType |
Journal Article
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