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 |
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| Authors: | Roppe Jeffrey R Wang Bowei Huang Dehua Tehrani Lida Kamenecka Theodore Schweiger Edwin J Anderson Jeffery J Brodkin Jesse Jiang Xiaohui Cramer Merryl Chung Janice Reyes-Manalo Grace Munoz Benito Cosford Nicholas D P |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. jeffrey_roppe@merck.com |
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| 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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