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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
18
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pubmed:dateCreated |
2000-12-26
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pubmed:abstractText |
Compounds containing a 1,2,3-triazole-substituted benzenesulfonamide were prepared and found to be potent and selective human beta3-adrenergic receptor agonists. The most interesting compound, trifluoromethylbenzyl analogue 12e (beta3 EC50 = 3.1 nM with >1500-fold selectivity over binding to both beta1- and beta2 receptors), stimulates lipolysis in the rhesus monkey (ED50 = 0.36 mg/kg) and is 25% orally bioavailable in the dog.
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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 |
Sep
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BrockunierL LLL,
pubmed-author:CandeloreM RMR,
pubmed-author:CascieriM AMA,
pubmed-author:ColwellL FLFJr,
pubmed-author:DenkHH,
pubmed-author:FeeneyW PWP,
pubmed-author:FisherM HMH,
pubmed-author:ForrestM JMJ,
pubmed-author:IRAG HGH,
pubmed-author:MacIntyreD EDE,
pubmed-author:OhH JHJ,
pubmed-author:ParmeeE RER,
pubmed-author:TothKK,
pubmed-author:WeberA EAE,
pubmed-author:WyvrattM JMJ
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pubmed:issnType |
Print
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pubmed:day |
18
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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 |
2111-4
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:10999482-Administration, Oral,
pubmed-meshheading:10999482-Adrenergic beta-3 Receptor Agonists,
pubmed-meshheading:10999482-Animals,
pubmed-meshheading:10999482-Biological Availability,
pubmed-meshheading:10999482-CHO Cells,
pubmed-meshheading:10999482-Cricetinae,
pubmed-meshheading:10999482-Cyclic AMP,
pubmed-meshheading:10999482-Dogs,
pubmed-meshheading:10999482-Dose-Response Relationship, Drug,
pubmed-meshheading:10999482-Humans,
pubmed-meshheading:10999482-Infusions, Parenteral,
pubmed-meshheading:10999482-Isoproterenol,
pubmed-meshheading:10999482-Lipolysis,
pubmed-meshheading:10999482-Macaca mulatta,
pubmed-meshheading:10999482-Protein Binding,
pubmed-meshheading:10999482-Receptors, Adrenergic, beta-3,
pubmed-meshheading:10999482-Structure-Activity Relationship,
pubmed-meshheading:10999482-Sulfonamides,
pubmed-meshheading:10999482-Tachycardia,
pubmed-meshheading:10999482-Triazoles
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pubmed:year |
2000
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pubmed:articleTitle |
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. linda_brockunier@merck.com
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pubmed:publicationType |
Journal Article,
Comparative Study
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