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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2008-1-21
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pubmed:abstractText |
Antagonism of the bradykinin B(1) receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating alpha-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B(1) receptor and good bioavailability in the rat and dog. In addition, these functionally active compounds show high passive permeability and low susceptibility to phosphoglycoprotein mediated efflux, predictive of good CNS exposure.
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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 |
1464-3405
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pubmed:author |
pubmed-author:AdaraynEmily DED,
pubmed-author:BednarRodney ARA,
pubmed-author:BockMark GMG,
pubmed-author:BohnDennis LDL,
pubmed-author:ChangRaymond S LRS,
pubmed-author:ChangRonald KRK,
pubmed-author:ClaytonFrank CFC,
pubmed-author:CookJacquelynn JJJ,
pubmed-author:CoxJ AJA,
pubmed-author:Di MarcoChristina NCN,
pubmed-author:DiPardoRobert MRM,
pubmed-author:FreidingerRoger MRM,
pubmed-author:HolahanMarie AMA,
pubmed-author:KimJune JJJ,
pubmed-author:KudukScott DSD,
pubmed-author:LemaireWeiW,
pubmed-author:LeonardYvonne MYM,
pubmed-author:MosserScott DSD,
pubmed-author:MurphyKathy LKL,
pubmed-author:PettiboneDouglas JDJ,
pubmed-author:PrueksaritanontThomayantT,
pubmed-author:RansomRichard WRW,
pubmed-author:SchirripaKathy MKM,
pubmed-author:SitkoGary RGR,
pubmed-author:TangCuyueC,
pubmed-author:WallaceAudrey AAA,
pubmed-author:WanBang-LinBL,
pubmed-author:WoodMichael RMR,
pubmed-author:YuJianJ
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pubmed:issnType |
Electronic
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pubmed:day |
15
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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 |
716-20
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pubmed:meshHeading |
pubmed-meshheading:18061443-Amides,
pubmed-meshheading:18061443-Animals,
pubmed-meshheading:18061443-Biological Availability,
pubmed-meshheading:18061443-Blood-Brain Barrier,
pubmed-meshheading:18061443-Cytochrome P-450 Enzyme System,
pubmed-meshheading:18061443-Dogs,
pubmed-meshheading:18061443-Half-Life,
pubmed-meshheading:18061443-Humans,
pubmed-meshheading:18061443-Rats,
pubmed-meshheading:18061443-Rats, Sprague-Dawley,
pubmed-meshheading:18061443-Receptor, Bradykinin B1,
pubmed-meshheading:18061443-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. michael_wood2@merck.com
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pubmed:publicationType |
Journal Article
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