摘要
如何使药物有效地穿越血脑屏障并发挥药效,是治疗中枢神经系统疾病的一大难题。通过结构修饰,可以改善小分子药物的理化性质,使其通过被动扩散的方式到达脑部;另外,可将药物修饰成能借助载体或受体介导的转运系统运输的结构,经由载/受体转运进入脑部。这两种手段是目前常用的改善药物血脑屏障通透性的化学方法。本文简要介绍了药物传送到脑部的主要途径,并重点阐述基于传送途径对小分子药物利用化学手段进行结构修饰以改善药物血脑屏障通透性的方法。
How to make drugs cross the blood-brain barrier and show therapeutic effects is the major challenge for the treatment of central nervous system diseases. The physicochemical properties of small molecular drugs can be improved through structure modification and the drugs can get to brain by means of passive diffusion. Drugs can also be modified to the structure which can be transported by carrier-mediated transport system or receptor-mediated transport system, reaching brain. These two chemical methods are common strategies currently to improve drug permeability of the blood-brain barrier. In this paper, the main ways of delivering drugs to brain will be briefly introduced and improving the permeability of small molecular drugs through structure modification will be reviewed.
出处
《中国药物化学杂志》
CAS
CSCD
2011年第6期489-494,506,共7页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(21102167)
关键词
血脑屏障
结构修饰
被动扩散
载体转运
blood-brain barrier
structure modification
passive diffusion
carrier-mediated transport
