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pubmed-article:19914063pubmed:abstractTextBased 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.lld:pubmed
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pubmed-article:19914063pubmed:copyrightInfoCopyright 2009 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:19914063pubmed:articleTitleDesign and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.lld:pubmed
pubmed-article:19914063pubmed:affiliationPfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, United States. kevin.k.liu@pfizer.comlld:pubmed
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