Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379071 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABAA agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABAAα2 and α3-subtypes and is anxiolytic in a conditioned animal model of anxiety with minimal sedation observed at full BZ binding site occupancy.
Graphical abstractImidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABAA agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABAAα2 and α3-subtypes and is anxiolytic in a conditioned animal model of anxiety with minimal sedation observed at full BZ binding site occupancy.Figure optionsDownload full-size imageDownload as PowerPoint slide