- 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.
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.
Bioorganic & medicinal chemistry letters (2004-07-01)
Jeffrey R Roppe, Bowei Wang, Dehua Huang, Lida Tehrani, Theodore Kamenecka, Edwin J Schweiger, Jeffery J Anderson, Jesse Brodkin, Xiaohui Jiang, Merryl Cramer, Janice Chung, Grace Reyes-Manalo, Benito Munoz, Nicholas D P Cosford
PMID15225713
RESUMEN
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.