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Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands |
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| Authors: | Arvanitis Argyrios G Rescinito Joseph T Arnold Charles R Wilde Richard G Cain Gary A Sun Jung Hui Yan Jia-Sheng Teleha Christopher A Fitzgerald Lawrence W McElroy John Zaczek Robert Hartig Paul R Grossman Scott Arneric Stephen P Gilligan Paul J Olson Richard E Robertson David W |
| Affiliation: | Discovery Chemistry-Wilmington, Bristol-Myers Squibb Company, Experimental Station, DE 19880, USA. argyrios.arvanitis@bms.com |
| Abstract: | 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. |
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