Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands
| Autor: | Argyrios G, Arvanitis, Joseph T, Rescinito, Charles R, Arnold, Richard G, Wilde, Gary A, Cain, Jung Hui, Sun, Jia-Sheng, Yan, Christopher A, Teleha, Lawrence W, Fitzgerald, John, McElroy, Robert, Zaczek, Paul R, Hartig, Scott, Grossman, Stephen P, Arneric, Paul J, Gilligan, Richard E, Olson, David W, Robertson |
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| Rok vydání: | 2003 |
| Předmět: |
Metabolic Clearance Rate
Pyridines Organic Chemistry Clinical Biochemistry Pharmaceutical Science Ligands Anxiety Disorders Receptors Corticotropin-Releasing Hormone Biochemistry Rats Structure-Activity Relationship Dogs Anti-Anxiety Agents Drug Discovery Animals Molecular Medicine Molecular Biology Half-Life |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 13:125-128 |
| ISSN: | 0960-894X |
| Popis: | 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 1mg/kg (po) and in the rat situational anxiety model to assess anxiolytic efficacy at 3mg/kg (po). The structure-activity relationships for good receptor binding affinity are described herein. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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