Peer-reviewed veterinary case report
Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2005
- Authors:
- St-Denis, Y et al.
- Affiliation:
- Department of Medicinal Chemistry · Italy
- Species:
- rodent
Abstract
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.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15946843/