474103-29-2Relevant academic research and scientific papers
Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety
St.-Denis,Di Fabio,Bernasconi,Castiglioni,Contini,Donati,Fazzolari,Gentile,Ghirlanda,Marchionni,Messina,Micheli,Pavone,Pasquarello,Sabbatini,Zampori,Arban,Vitulli
, p. 3713 - 3716 (2007/10/03)
Two isomers of the hexahydro-tetraazaacenaphthylene templates (1 and 2) are presented as novel, potent, and selective corticotropin releasing factor-1 (CRF1) receptor antagonists. In this paper, we report the affinity and SAR of a series of compounds, as well as pharmacokinetic characterization of a chosen set. The anxiolitic activity of a selected example (2ba) in the rat pup vocalization model is also presented.
