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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2011-3-17
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pubmed:abstractText |
The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.
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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 |
Mar
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BoninPaul DPD,
pubmed-author:ChenYueY,
pubmed-author:CorneliusPeterP,
pubmed-author:DaroutEtzerE,
pubmed-author:DeNinnoMichael PMP,
pubmed-author:FutatsugiKentaroK,
pubmed-author:GuimarãesCristiano R WCR,
pubmed-author:HarrisAnthony RAR,
pubmed-author:HornbySamS,
pubmed-author:KalgutkarAmit SAS,
pubmed-author:KohrtJeffreyJ,
pubmed-author:KungDanielD,
pubmed-author:LefkerBruce ABA,
pubmed-author:LiBryanB,
pubmed-author:MascittiVincentV,
pubmed-author:McClureKim FKF,
pubmed-author:MooreDianna EDE,
pubmed-author:MunchhofMichael JMJ,
pubmed-author:RobinsonRalph PRP,
pubmed-author:SalterEbenE,
pubmed-author:SampLaceyL,
pubmed-author:WangRuduanR
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pubmed:issnType |
Electronic
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pubmed:day |
24
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pubmed:volume |
54
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pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
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pubmed:pagination |
1948-52
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pubmed:meshHeading |
pubmed-meshheading:21361292-Animals,
pubmed-meshheading:21361292-Azabicyclo Compounds,
pubmed-meshheading:21361292-Glucose Tolerance Test,
pubmed-meshheading:21361292-Humans,
pubmed-meshheading:21361292-Molecular Conformation,
pubmed-meshheading:21361292-Pyrimidines,
pubmed-meshheading:21361292-Rats,
pubmed-meshheading:21361292-Receptors, G-Protein-Coupled,
pubmed-meshheading:21361292-Species Specificity,
pubmed-meshheading:21361292-Stereoisomerism,
pubmed-meshheading:21361292-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
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pubmed:affiliation |
Department of Medicinal Chemistry, Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States. kim.f.mcclure@pfizer.com
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pubmed:publicationType |
Journal Article,
Comparative Study
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