rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
13
|
pubmed:dateCreated |
2000-10-11
|
pubmed:abstractText |
5-n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and selective beta3 adrenergic receptor agonist (beta3 EC50 = 23 nM, beta1 IC50 = 3000 nM, beta2 IC50 = 3000 nM). The compound has high oral bioavailability in dogs (62%) and rats (36%) and is among the most orally bioavailable beta3 adrenergic receptor agonists reported to date.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jul
|
pubmed:issn |
0960-894X
|
pubmed:author |
pubmed-author:BiftuTT,
pubmed-author:CandeloreM RMR,
pubmed-author:CascieriM AMA,
pubmed-author:ColwellL FLFJr,
pubmed-author:DenkHH,
pubmed-author:FeeneyW PWP,
pubmed-author:FengD DDD,
pubmed-author:FisherM HMH,
pubmed-author:ForrestM JMJ,
pubmed-author:IRAG HGH,
pubmed-author:MacIntyreD EDE,
pubmed-author:MillerR RRR,
pubmed-author:StearnsR ARA,
pubmed-author:StraderC DCD,
pubmed-author:TothKK,
pubmed-author:WeberA EAE,
pubmed-author:WyvrattM JMJ
|
pubmed:issnType |
Print
|
pubmed:day |
3
|
pubmed:volume |
10
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1427-9
|
pubmed:dateRevised |
2010-11-18
|
pubmed:meshHeading |
pubmed-meshheading:10888324-Administration, Oral,
pubmed-meshheading:10888324-Adrenergic beta-3 Receptor Agonists,
pubmed-meshheading:10888324-Adrenergic beta-Agonists,
pubmed-meshheading:10888324-Animals,
pubmed-meshheading:10888324-Biological Availability,
pubmed-meshheading:10888324-CHO Cells,
pubmed-meshheading:10888324-Cricetinae,
pubmed-meshheading:10888324-Dogs,
pubmed-meshheading:10888324-Drug Design,
pubmed-meshheading:10888324-Humans,
pubmed-meshheading:10888324-Molecular Structure,
pubmed-meshheading:10888324-Oxadiazoles,
pubmed-meshheading:10888324-Rats,
pubmed-meshheading:10888324-Structure-Activity Relationship
|
pubmed:year |
2000
|
pubmed:articleTitle |
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
|
pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway NJ 07065, USA. danqing_feng@merck.com
|
pubmed:publicationType |
Journal Article
|