Source:http://linkedlifedata.com/resource/pubmed/id/11720857
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
24
|
| pubmed:dateCreated |
2001-11-26
|
| pubmed:abstractText |
The preparation and structure-activity relationships (SARs) of potent agonists of the human beta(3)-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human beta(3)-AR potency with selectivity over human beta(1)-AR and/or human beta(2)-AR agonism. Compound 29s was identified as a potent (EC(50)=1nM) and selective (greater than 400-fold over beta(1)- with no beta(2)-AR agonism) full beta(3)-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Dec
|
| pubmed:issn |
0960-894X
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
17
|
| pubmed:volume |
11
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
3123-7
|
| pubmed:dateRevised |
2010-11-18
|
| pubmed:meshHeading |
pubmed-meshheading:11720857-Adrenergic beta-3 Receptor Agonists,
pubmed-meshheading:11720857-Adrenergic beta-Agonists,
pubmed-meshheading:11720857-Animals,
pubmed-meshheading:11720857-Humans,
pubmed-meshheading:11720857-Mice,
pubmed-meshheading:11720857-Mice, Transgenic,
pubmed-meshheading:11720857-Piperidines,
pubmed-meshheading:11720857-Urea
|
| pubmed:year |
2001
|
| pubmed:articleTitle |
4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor.
|
| pubmed:affiliation |
Chemical Sciences, Wyeth-Ayerst Research, PO Box CN-8000, USA. mashwell@arqule.com
|
| pubmed:publicationType |
Journal Article
|