See today's edition of
DailyUpdates in your
therapeutic area
Search all articles

Keywords:

Boolean terms AND, OR, NOT can be used. Phrases should be entered within quotes. For wildcards use an *

Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF(1) receptor antagonists.

Bioorganic & medicinal chemistry letters 2007 Jun 30; 17(18):5218-21

Link to PubMed abstract

Gentile G G, Di Fabio R R, Pavone F F, Sabbatini F FM, St-Denis Y Y, Zampori M MG,

Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithkline, Medicine Research Centre, Via F

Corticotropin-releasing factor (CRF), a 41 amino acid peptide neurohormone synthesised by specific hypothalamic nuclei in the brain, is implicated in stress-related function. Antagonism of CRF(1) receptors is an attractive therapeutic approach for the treatment of depression and anxiety. Unsaturated tetrahydrotriazaacenaphthylenes of general structure 3 have been identified as potent and selective CRF(1) receptor antagonists with a suitable oral pharmacokinetic profile.