Minimizing Drug Exposure in the CNS while Maintaining Good Oral Absorption

被引：14

作者：

Bagal, Sharan K. ^{[1
]}

Bungay, Peter J. ^{[1
]}

机构：

[1] Pfizer Neusentis, Cambridge CB21 6GS, England

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2012年 / 3卷 / 12期

关键词：

BRAIN PENETRATION;

D O I：

10.1021/ml300378n

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

In some drug discovery approaches, it is advantageous to restrict the access of compounds to the CNS to minimize the risk of side effects. By choosing appropriate physicochemical properties and building in the ability to act as substrates for active efflux transporters, it is possible to achieve CNS restriction and still retain sufficient absorption through the intestinal epithelium to retain good oral bioavailability. Potential risks in employing this approach are considered.

引用

收藏

页码：948 / 950

页数：3

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