| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377553 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
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 CRF1 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 CRF1 receptor antagonists with a suitable oral pharmacokinetic profile.
Graphical abstractNovel unsaturated tetrahydrotriazaacenaphthylenes have been identified as potent and selective CRF1 receptor antagonists showing good oral pharmacokinetic profile in rats.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Authors
Gabriella Gentile, Romano Di Fabio, Francesca Pavone, Fabio Maria Sabbatini, Yves St-Denis, Maria Grazia Zampori, Giovanni Vitulli, Angela Worby,