GLUT1高亲和力的脑靶向文拉法辛前药的设计和合成
esign and Synthesis of Brain Targeted Prodrug of Venlafaxine With GLUT1 High Affinity
为了提高抗抑郁药文拉法辛的脑靶向性，本文选择了血脑屏障上的葡萄糖转运蛋白1为靶标，设计并合成了一系列脑靶向性的文拉法辛前药1。文中以文拉法辛为起始原料，通过桥链与三甲硅基保护的葡萄糖偶联，脱去保护基，得到目标化合物1，经H NMR、IR和MS确证结构。
In this paper a series of brain-targeting Venlafaxine prodrugs utilizing the glucose transporter member 1 (GLUT1) was discribed. Venlafaxine used as starting material was conjugated with 1,2,3,4-tetra-O-trimethysilyl-D-glucopyranose by different bicarboxyl acid, and then deprotected to afford the targeting compounds 1 which were conformed by H NMR, IR and MS.
任云、海俐、吴勇
药学生物化学
药物化学葡萄糖转运体1脑靶向前药合成
Medicinal chemistryglucose transporter 1brain targetingprodrugsynthesis
任云,海俐,吴勇.GLUT1高亲和力的脑靶向文拉法辛前药的设计和合成[EB/OL].(2012-07-03)[2025-08-02].http://www.paper.edu.cn/releasepaper/content/201207-44.点此复制
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