环状苯甲脒作为口服有效的NR2B选择性NMDA受体拮抗剂。
Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists.
作者信息
Nguyen Kevin T, Claiborne Christopher F, McCauley John A, Libby Brian E, Claremon David A, Bednar Rodney A, Mosser Scott D, Gaul Stanley L, Connolly Thomas M, Condra Cindra L, Bednar Bohumil, Stump Gary L, Lynch Joseph J, Koblan Kenneth S, Liverton Nigel J
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3997-4000. doi: 10.1016/j.bmcl.2007.04.084. Epub 2007 Apr 29.
PMID:17498948
Abstract
A novel series of cyclic benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 29 is orally active in a carrageenan-induced rat hyperalgesia model of pain.
摘要
合成了一系列新型环状苯甲脒，并显示出具有NR2B亚型选择性NMDA拮抗剂活性。化合物29在角叉菜胶诱导的大鼠疼痛性痛觉过敏模型中具有口服活性。
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