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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2000-10-11
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pubmed:abstractText |
Benzyl and phenoxymethylene substituted oxadiazoles are potent and orally bioavailable beta3 adrenergic receptor (AR) agonists. The 4-trifluormethoxy substituted 5-benzyl oxadiazole 5f has an EC50 of 8 nM in the beta3 AR agonist assay with 100-fold selectivity over beta1 and beta2 AR binding inhibition activity. Its oral bioavailability in dogs is 30 +/- 4%, with a half-life of 3.8 +/- 0.4 h. In the anesthetized rhesus, 5f evoked a dose-dependent glycerolemia (ED50Gly = 0.15 mg/kg). Under these conditions a heart rate increase of 15% was observed at a dose level of 10 mg/kg.
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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 |
Jul
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BiftuTT,
pubmed-author:CandeloreM RMR,
pubmed-author:CascieriM AMA,
pubmed-author:ColandreaV JVJ,
pubmed-author:ColwellL FLFJr,
pubmed-author:FengD DDD,
pubmed-author:FisherM HMH,
pubmed-author:ForrestM JMJ,
pubmed-author:IRAG HGH,
pubmed-author:KunII,
pubmed-author:LiangG BGB,
pubmed-author:MacIntyreD EDE,
pubmed-author:NaylorE MEM,
pubmed-author:QianXX,
pubmed-author:StearnsR ARA,
pubmed-author:StraderC DCD,
pubmed-author:WeberA EAE,
pubmed-author:WyvrattM JMJ
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pubmed:issnType |
Print
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pubmed:day |
3
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1431-4
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:10888325-Adrenergic beta-3 Receptor Agonists,
pubmed-meshheading:10888325-Adrenergic beta-Agonists,
pubmed-meshheading:10888325-Animals,
pubmed-meshheading:10888325-Anti-Obesity Agents,
pubmed-meshheading:10888325-Biological Availability,
pubmed-meshheading:10888325-CHO Cells,
pubmed-meshheading:10888325-Cricetinae,
pubmed-meshheading:10888325-Dogs,
pubmed-meshheading:10888325-Drug Design,
pubmed-meshheading:10888325-Glycerol,
pubmed-meshheading:10888325-Heart Rate,
pubmed-meshheading:10888325-Humans,
pubmed-meshheading:10888325-Macaca mulatta,
pubmed-meshheading:10888325-Oxadiazoles,
pubmed-meshheading:10888325-Structure-Activity Relationship,
pubmed-meshheading:10888325-Sulfonamides
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pubmed:year |
2000
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pubmed:articleTitle |
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. tesfaye_biftu@merck.com
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pubmed:publicationType |
Journal Article
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