Imidazo[4,5- b]pyridines as corticotropin releasing factor receptor ligands
A series of high affinity CRF receptor ligands with an imidazo[4,5- b]pyridine core is described. Individual analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were further tested in the dog N-in-1 pharmacokinetic model to assess plasma levels at 1 mg/kg (p...
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Published in | Bioorganic & medicinal chemistry letters Vol. 13; no. 1; pp. 125 - 128 |
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Main Authors | , , , , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
06.01.2003
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | A series of high affinity CRF receptor ligands with an imidazo[4,5-
b]pyridine core is described. Individual analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were further tested in the dog N-in-1 pharmacokinetic model to assess plasma levels at 1
mg/kg (po) and in the rat situational anxiety model to assess anxiolytic efficacy at 3
mg/kg (po). The structure–activity relationships for good receptor binding affinity are described herein.
A series of high affinity CRF receptor ligands with an imidazo[4,5-
b]pyridine core is described. Analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were tested in the dog N-in-1 pharmacokinetic at 1
mg/kg (po) and in the rat situational anxiety model at 3
mg/kg (po). |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(02)00833-8 |