Peer-reviewed veterinary case report
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2004
- Authors:
- Roppe, Jeffrey R et al.
- Affiliation:
- Department of Medicinal Chemistry · United States
- Species:
- rodent
Abstract
Structure-activity relationship studies leading to the discovery of a new, orally active mGlu5 receptor antagonist are described. The title compound, 5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine, is highly potent in vitro, has good in vivo receptor occupancy, and is efficacious in the rat fear-potentiated startle model of anxiety following oral dosing.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15225713/