Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands
摘要:
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 pharmaco-kinetic 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. (C) 2002 Elsevier Science Ltd. All rights reserved.
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands
摘要:
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 pharmaco-kinetic 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. (C) 2002 Elsevier Science Ltd. All rights reserved.
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands
作者: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
DOI:10.1016/s0960-894x(02)00833-8
日期:2003.1
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 pharmaco-kinetic 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. (C) 2002 Elsevier Science Ltd. All rights reserved.