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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2009-4-16
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pubmed:abstractText |
A novel 4-hydroxyl(diphenyl)methyl substituted quinuclidine series was discovered as a very promising class of muscarinic antagonists. The structure-activity relationships of the connectivity of the diphenyl moiety to the quinuclidine core and around the ring nitrogen side chain are described. Computational docking studies using an homology model of the M(3) receptor readily explained the observed structure-activity relationship of the various compounds. Compound 14o was identified as a very potent, slowly reversible M(3) antagonist with a very long in vivo duration of bronchoprotection.
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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 |
Apr
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BelmonteKristenK,
pubmed-author:BlaneyFrank EFE,
pubmed-author:BurmanMiriamM,
pubmed-author:DufourJeremyJ,
pubmed-author:FoleyJames JJJ,
pubmed-author:LainéDramane IDI,
pubmed-author:LuttmannMark AMA,
pubmed-author:McClelandBrentB,
pubmed-author:NeippChristopherC,
pubmed-author:PalovichMichael RMR,
pubmed-author:SalmonMichaelM,
pubmed-author:ThomasSoniaS,
pubmed-author:UnderwoodBrianB,
pubmed-author:WebbEdward FEF,
pubmed-author:WiddowsonKatherine LKL
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pubmed:issnType |
Electronic
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pubmed:day |
23
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2493-505
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pubmed:dateRevised |
2009-8-13
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pubmed:meshHeading |
pubmed-meshheading:19317446-Animals,
pubmed-meshheading:19317446-Benzhydryl Compounds,
pubmed-meshheading:19317446-Biological Availability,
pubmed-meshheading:19317446-Bronchi,
pubmed-meshheading:19317446-Bronchoconstriction,
pubmed-meshheading:19317446-Bronchodilator Agents,
pubmed-meshheading:19317446-CHO Cells,
pubmed-meshheading:19317446-Calcium,
pubmed-meshheading:19317446-Cricetinae,
pubmed-meshheading:19317446-Cricetulus,
pubmed-meshheading:19317446-Humans,
pubmed-meshheading:19317446-Mice,
pubmed-meshheading:19317446-Models, Molecular,
pubmed-meshheading:19317446-Muscle, Smooth,
pubmed-meshheading:19317446-Muscle Contraction,
pubmed-meshheading:19317446-Quinuclidines,
pubmed-meshheading:19317446-Radioligand Assay,
pubmed-meshheading:19317446-Rats,
pubmed-meshheading:19317446-Receptor, Muscarinic M3,
pubmed-meshheading:19317446-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.
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pubmed:affiliation |
GlaxoSmithKline, Respiratory CEDD, 709 Swedeland Road, P.O. Box 1539, King of Prussia, Pennsylvania 19406-0939, USA. dramane.i.laine@gsk.com
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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