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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2003-5-1
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pubmed:abstractText |
Antagonism of the bradykinin B(1) receptor was demonstrated to be a potential treatment for chronic pain and inflammation. Novel benzodiazepines were designed that display subnanomolar affinity for the bradykinin B(1) receptor (K(i) = 0.59 nM) and high selectivity against the bradykinin B(2) receptor (K(i) > 10 microM). In vivo efficacy, comparable to morphine, was demonstrated for lead compounds in a rodent hyperalgesia model.
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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 |
May
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BockMark GMG,
pubmed-author:BondiskeyPeter JPJ,
pubmed-author:ChangRaymond S LRS,
pubmed-author:ChenTsing-BauTB,
pubmed-author:DiPardoRobert MRM,
pubmed-author:DorseyBruce DBD,
pubmed-author:EllisJoan DJD,
pubmed-author:FreidingerRoger MRM,
pubmed-author:HarrellCharles MCM,
pubmed-author:HomnickCarl FCF,
pubmed-author:KimJune JJJ,
pubmed-author:KudukScott DSD,
pubmed-author:LisEdward VEV,
pubmed-author:LynchJoseph JJJ,
pubmed-author:MacNeilTanyaT,
pubmed-author:MillerPatricia JPJ,
pubmed-author:MurphyKathy LKL,
pubmed-author:O'MalleyStacey SSS,
pubmed-author:PettiboneDouglas JDJ,
pubmed-author:RansomRichard WRW,
pubmed-author:SandhuPunamP,
pubmed-author:StumpGary LGL,
pubmed-author:VosJ JJJ,
pubmed-author:WoodMichael RMR
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pubmed:issnType |
Print
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pubmed:day |
8
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1803-6
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:12723943-Animals,
pubmed-meshheading:12723943-Benzodiazepines,
pubmed-meshheading:12723943-CHO Cells,
pubmed-meshheading:12723943-Cricetinae,
pubmed-meshheading:12723943-Humans,
pubmed-meshheading:12723943-Hyperalgesia,
pubmed-meshheading:12723943-Radioligand Assay,
pubmed-meshheading:12723943-Rats,
pubmed-meshheading:12723943-Rats, Sprague-Dawley,
pubmed-meshheading:12723943-Receptor, Bradykinin B1,
pubmed-meshheading:12723943-Receptor, Bradykinin B2,
pubmed-meshheading:12723943-Receptors, Bradykinin,
pubmed-meshheading:12723943-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
Benzodiazepines as potent and selective bradykinin B1 antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 4, West Point, Pennsylvania 19486, USA. michael_wood2@merck.com
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pubmed:publicationType |
Journal Article
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