5-[(2-甲基-1,3-噻唑-4-基)乙炔基]-2,3'-联吡啶：一种高效、口服活性的代谢型谷氨酸5（mGlu5）受体拮抗剂，具有抗焦虑活性。
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.
作者信息
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
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA.
出版信息
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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