Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists |
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| Authors: | Gentile Gabriella Di Fabio Romano Pavone Francesca Sabbatini Fabio Maria St-Denis Yves Zampori Maria Grazia Vitulli Giovanni Worby Angela |
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| Affiliation: | Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithkline, Medicine Research Centre, Via Fleming 4, 37135 Verona, Italy. gg87301@gsk.com |
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| Abstract: | 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. |
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