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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2001-11-20
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pubmed:abstractText |
A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 (25), a potent beta(3) full agonist (K(i)=21 nM, 95% activation) with partial agonist (45%) activity at the beta(1) receptor. Based on its desirable in vitro and in vivo properties, BMS-196085 was chosen for clinical evaluation.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-1 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-3 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Anilides,
http://linkedlifedata.com/resource/pubmed/chemical/Blood Glucose,
http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-3
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:Abboa-OffeiB EBE,
pubmed-author:AllenG TGT,
pubmed-author:ArbeenyC MCM,
pubmed-author:BednarzM SMS,
pubmed-author:CatII,
pubmed-author:CiosekC PCPJr,
pubmed-author:DickinsonK EKE,
pubmed-author:FisherL GLG,
pubmed-author:FrohlichB HBH,
pubmed-author:GavaiA VAV,
pubmed-author:GeorgeR JRJ,
pubmed-author:GirotraR NRN,
pubmed-author:HarperT WTW,
pubmed-author:HillyerD EDE,
pubmed-author:MathurAA,
pubmed-author:McCannP JPJ,
pubmed-author:MikkilineniA BAB,
pubmed-author:PossK MKM,
pubmed-author:RoyA CAC,
pubmed-author:SeymourA AAA,
pubmed-author:SherP MPM,
pubmed-author:SkwishSS,
pubmed-author:SlusarchykD ADA,
pubmed-author:TesfamariamBB,
pubmed-author:WaldronT LTL,
pubmed-author:WangT CTC,
pubmed-author:WashburnW NWN,
pubmed-author:WuGG,
pubmed-author:YoungD ADA
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pubmed:issnType |
Print
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pubmed:day |
3
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pubmed:volume |
11
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3041-4
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:11714606-Administration, Oral,
pubmed-meshheading:11714606-Adrenergic Agonists,
pubmed-meshheading:11714606-Adrenergic beta-1 Receptor Agonists,
pubmed-meshheading:11714606-Adrenergic beta-3 Receptor Agonists,
pubmed-meshheading:11714606-Anilides,
pubmed-meshheading:11714606-Animals,
pubmed-meshheading:11714606-Blood Glucose,
pubmed-meshheading:11714606-Cercopithecus aethiops,
pubmed-meshheading:11714606-Drug Evaluation, Preclinical,
pubmed-meshheading:11714606-Fatty Acids,
pubmed-meshheading:11714606-Humans,
pubmed-meshheading:11714606-Mice,
pubmed-meshheading:11714606-Mice, Obese,
pubmed-meshheading:11714606-Receptors, Adrenergic, beta-1,
pubmed-meshheading:11714606-Receptors, Adrenergic, beta-3,
pubmed-meshheading:11714606-Structure-Activity Relationship
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pubmed:year |
2001
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pubmed:articleTitle |
BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
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pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. ashvinikumar.gavai@bms.com
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pubmed:publicationType |
Journal Article
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