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ID: ALA1136411
Journal: Bioorg Med Chem Lett
Title: Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
Authors: Arvanitis AG, Rescinito JT, Arnold CR, Wilde RG, Cain GA, Sun JH, Yan JS, Teleha CA, Fitzgerald LW, McElroy J, Zaczek R, Hartig PR, Grossman S, Arneric SP, Gilligan PJ, Olson RE, Robertson DW.
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.
CiteXplore: 12467631