Author/Authors :
Argyrios G. Arvanitis، نويسنده , , Joseph T. Rescinito، نويسنده , , Charles R. Arnold، نويسنده , , Richard G. Wilde، نويسنده , , Gary A. Cain، نويسنده , , Jung-Hui Sun، نويسنده , , Jia-Sheng Yan، نويسنده , , Christopher A. Teleha، نويسنده , , Lawrence W. Fitzgerald، نويسنده , , John McElroy، نويسنده , , Robert Zaczek، نويسنده , , Paul R. Hartig، نويسنده , , Scott Grossman، نويسنده , , Stephen P. Arneric، نويسنده , , Paul J. Gilligan، نويسنده , , Richard E. Olson، نويسنده , , David W. Robertson، نويسنده ,
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 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.
