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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2003-3-26
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pubmed:abstractText |
A novel series of 2-(3-indolyl)alkylamino-1-(3-chlorophenyl)ethanols was prepared and evaluated for in vitro ability to stimulate cAMP production in Chinese hamster ovary cells expressing cloned human beta(3)-AR. The optically active 30a was found to be the most potent and selective human beta(3)-AR agonist in this series with an EC(50) value of 0.062nM. In addition, 30a selectivity for human beta(3)-AR was 210-fold and 103-fold that for human beta(2)-AR and beta(1)-AR, respectively. Furthermore, 30a showed potent agonistic activity at rat beta(3)-AR.
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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 |
Apr
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1301-5
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:12657269-Adrenergic beta-3 Receptor Agonists,
pubmed-meshheading:12657269-Adrenergic beta-Agonists,
pubmed-meshheading:12657269-Alkanes,
pubmed-meshheading:12657269-Animals,
pubmed-meshheading:12657269-CHO Cells,
pubmed-meshheading:12657269-Cloning, Molecular,
pubmed-meshheading:12657269-Cricetinae,
pubmed-meshheading:12657269-Cyclic AMP,
pubmed-meshheading:12657269-Ethanolamines,
pubmed-meshheading:12657269-Humans,
pubmed-meshheading:12657269-Indoles,
pubmed-meshheading:12657269-Models, Molecular,
pubmed-meshheading:12657269-Molecular Conformation,
pubmed-meshheading:12657269-Rats,
pubmed-meshheading:12657269-Structure-Activity Relationship,
pubmed-meshheading:12657269-Tryptamines
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pubmed:year |
2003
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pubmed:articleTitle |
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.
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pubmed:affiliation |
Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Enoki, Suita, Japan. hiroshi-harada@dainippon-pharm.co.jp
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pubmed:publicationType |
Journal Article
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