Title of article :
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
Author/Authors :
Jeffrey R Roppe، نويسنده , , Bowei Wang، نويسنده , , Dehua Huang، نويسنده , , Lida Tehrani، نويسنده , , Theodore Kamenecka، نويسنده , , Edwin J. Schweiger، نويسنده , , Jeffery J Anderson، نويسنده , , Jesse Brodkin، نويسنده , , Xiaohui Jiang، نويسنده , , Merryl Cramer، نويسنده , , Janice Chung، نويسنده , , Grace Reyes-Manalo، نويسنده , , Benito Munoz، نويسنده , , Nicholas D.P Cosford، نويسنده ,
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.
Keywords :
metabotropic glutamate receptor , mGluR , MPEP , MTEP. , mGluR5
