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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
1999-1-25
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pubmed:abstractText |
A cloned human beta 3 adrenergic receptor assay was used to identify phenoxypropanolamine agonist 1. SAR studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM beta 3 agonist which shows 30-fold selectivity for beta 3 agonist activity over beta 1 and beta 2 receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over beta 1 and beta 2, respectively.
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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 beta-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/CGP 12177,
http://linkedlifedata.com/resource/pubmed/chemical/Propanolamines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-2,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-3,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/benzenesulfonamide
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pubmed:status |
MEDLINE
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pubmed:month |
May
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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 |
5
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1101-6
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:9871716-Adrenergic beta-Agonists,
pubmed-meshheading:9871716-Cloning, Molecular,
pubmed-meshheading:9871716-Drug Design,
pubmed-meshheading:9871716-Humans,
pubmed-meshheading:9871716-Molecular Conformation,
pubmed-meshheading:9871716-Molecular Structure,
pubmed-meshheading:9871716-Propanolamines,
pubmed-meshheading:9871716-Receptors, Adrenergic, beta,
pubmed-meshheading:9871716-Receptors, Adrenergic, beta-1,
pubmed-meshheading:9871716-Receptors, Adrenergic, beta-2,
pubmed-meshheading:9871716-Receptors, Adrenergic, beta-3,
pubmed-meshheading:9871716-Recombinant Proteins,
pubmed-meshheading:9871716-Stereoisomerism,
pubmed-meshheading:9871716-Structure-Activity Relationship,
pubmed-meshheading:9871716-Sulfonamides
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pubmed:year |
1998
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pubmed:articleTitle |
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
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pubmed:publicationType |
Journal Article
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