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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose-responsive in vivo efficacy in our pre-clinical food intake 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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BrownJaniceJ,
pubmed-author:CorneliusPeterP,
pubmed-author:GibbonsColleenC,
pubmed-author:GohY TYT,
pubmed-author:KongJimmy XJX,
pubmed-author:LeeEunsunE,
pubmed-author:LiuKevin K-CKK,
pubmed-author:MaralaRaviR,
pubmed-author:MaurerTristan STS,
pubmed-author:PattersonTerrell ATA,
pubmed-author:SantucciStephanieS,
pubmed-author:TomlinsonElizabethE,
pubmed-author:VageChandraC,
pubmed-author:WenzelZaneZ,
pubmed-author:WernerWendyW
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pubmed:copyrightInfo |
Copyright 2009 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 |
266-71
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:19914063-Administration, Oral,
pubmed-meshheading:19914063-Animals,
pubmed-meshheading:19914063-Anti-Obesity Agents,
pubmed-meshheading:19914063-Aza Compounds,
pubmed-meshheading:19914063-Dogs,
pubmed-meshheading:19914063-Drug Design,
pubmed-meshheading:19914063-Haplorhini,
pubmed-meshheading:19914063-Humans,
pubmed-meshheading:19914063-Obesity,
pubmed-meshheading:19914063-Rats,
pubmed-meshheading:19914063-Receptor, Serotonin, 5-HT2C,
pubmed-meshheading:19914063-Serotonin 5-HT2 Receptor Agonists,
pubmed-meshheading:19914063-Serotonin Receptor Agonists
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pubmed:year |
2010
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pubmed:articleTitle |
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.
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pubmed:affiliation |
Pfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, United States. kevin.k.liu@pfizer.com
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pubmed:publicationType |
Journal Article
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