512847-47-1Relevant articles and documents
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin- 3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists
Dzierba, Carolyn D.,Sielecki, Thais M.,Arvanitis, Argyrios G.,Galka, Amy,Johnson, Tricia L.,Takvorian, Amy G.,Rafalski, Maria,Kasireddy-Polam, Padmaja,Vig, Shikha,Dasgupta, Bireshwar,Zhang, Ge,Molski, Thaddeus F.,Wong, Harvey,Zaczek, Robert C.,Lodge, Nicholas J.,Combs, Andrew P.,Gilligan, Paul J.,Trainor, George L.,Bronson, Joanne J.,MacOr, John E.
, p. 4986 - 4989 (2012/08/28)
Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
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
, p. 125 - 128 (2007/10/03)
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.
