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
Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6. doi: 10.1016/j.bmcl.2004.05.037.
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.
本文描述了结构-活性关系研究，该研究导致发现了一种新型的口服活性代谢型谷氨酸受体5（mGlu5）拮抗剂。标题化合物5-[(2-甲基-1,3-噻唑-4-基)乙炔基]-2,3'-联吡啶在体外具有高效力，在体内具有良好的受体占有率，并且在口服给药后的大鼠焦虑恐惧增强惊吓模型中有效。
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