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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2005-8-4
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pubmed:abstractText |
The synthesis and SAR studies of tricyclic imidazo[4,5-b]pyridin-2-ones as human corticotropin-releasing factor receptor (CRF(1)) antagonists are discussed herein. Compound 16g was identified as a functional antagonist that inhibited CRF-stimulated cyclic adenosine monophosphate production and CRF-induced adrenocorticotrophic hormone release. Pharmacokinetics studies in rats showed that 16g was orally bioavailable, had good brain penetration, and had a moderate half-life. In our effort to identify CRF(1) antagonists with improved pharmacokinetics properties, 16g exhibited a favorably lower volume of distribution.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:ChenTa KungTK,
pubmed-author:CrowePaul DPD,
pubmed-author:DyckBrianB,
pubmed-author:GreyJonathanJ,
pubmed-author:GrigoriadisDimitri EDE,
pubmed-author:GrossRaymond SRS,
pubmed-author:GuoZhiqiangZ,
pubmed-author:HaddachMustaphaM,
pubmed-author:KiankarimiMehrakM,
pubmed-author:LanierMarionM,
pubmed-author:LiBin-FengBF,
pubmed-author:LuoZhiyongZ,
pubmed-author:McCarthyJames RJR,
pubmed-author:MoorjaniManishaM,
pubmed-author:SaundersJohnJ,
pubmed-author:SullivanRobertR,
pubmed-author:TellewJohn EJE,
pubmed-author:WilliamsJohn PJP,
pubmed-author:Zamani-KordSaidS,
pubmed-author:ZhangXiaohuX
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pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5104-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16078829-Administration, Oral,
pubmed-meshheading:16078829-Adrenocorticotropic Hormone,
pubmed-meshheading:16078829-Animals,
pubmed-meshheading:16078829-Blood-Brain Barrier,
pubmed-meshheading:16078829-CHO Cells,
pubmed-meshheading:16078829-Corticotropin-Releasing Hormone,
pubmed-meshheading:16078829-Cricetinae,
pubmed-meshheading:16078829-Cricetulus,
pubmed-meshheading:16078829-Cyclic AMP,
pubmed-meshheading:16078829-Drug Design,
pubmed-meshheading:16078829-Heterocyclic Compounds, 3-Ring,
pubmed-meshheading:16078829-Humans,
pubmed-meshheading:16078829-Imidazoles,
pubmed-meshheading:16078829-Injections, Intravenous,
pubmed-meshheading:16078829-Male,
pubmed-meshheading:16078829-Pyridines,
pubmed-meshheading:16078829-Radioligand Assay,
pubmed-meshheading:16078829-Rats,
pubmed-meshheading:16078829-Rats, Sprague-Dawley,
pubmed-meshheading:16078829-Receptors, Corticotropin-Releasing Hormone,
pubmed-meshheading:16078829-Stereoisomerism,
pubmed-meshheading:16078829-Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. zguo@neurocrine.com
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pubmed:publicationType |
Journal Article
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