2-（2-[3-（吡啶-3-基氧基）苯基]-2H-四氮唑-5-基）吡啶：一种高效、口服活性的代谢型谷氨酸受体5（mGlu5）拮抗剂。
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
作者信息
Huang Dehua, Poon Steve F, Chapman Deborah F, Chung Janice, Cramer Merryl, Reger Thomas S, Roppe Jeffrey R, Tehrani Lida, Cosford Nicholas D P, Smith Nicholas D
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2004 Nov 15;14(22):5473-6. doi: 10.1016/j.bmcl.2004.09.012.
Structure-activity relationship studies on 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery of 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl)pyridine (10)-a highly potent and selective mGlu5 receptor antagonist with good brain penetration and in vivo receptor occupancy in rat and cross-species oral bioavailability.
对3-(5-吡啶-2-基-2H-四氮唑-2-基)苯甲腈2的构效关系研究导致发现了2-(2-[3-(吡啶-3-基氧基)苯基]-2H-四氮唑-5-基)吡啶(10)——一种高效且选择性的mGlu5受体拮抗剂，具有良好的脑渗透性、大鼠体内受体占有率以及跨物种口服生物利用度。
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