High throughput artificial membrane permeability assay for blood-brain barrier

被引：970
作者：
Di, L
Kerns, EH
Fan, K
McConnell, OJ
Carter, GT
机构：
[1] Wyeth Res, Discovery Analyt Chem, Chem Sci, Princeton, NJ 08543 USA
[2] Wyeth Res, Biol Chem, Princeton, NJ 08543 USA
[3] Wyeth Res, Discovery Analyt Chem, Chem Sci, Pearl River, NY 10965 USA
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 38卷 / 03期
关键词：
artificial membrane; permeability; PAMPA; blood-brain barrier; brain penetration; CNS;
D O I：
10.1016/S0223-5234(03)00012-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The recent advances in high throughput screening for biological activities and combinatorial chemistry have greatly expanded the number of drug candidates. Rapid screening for BBB penetration potential early in drug discovery programs provides important information for compound selection and guidance of synthesis for desirable CNS properties. In this paper, we discuss a modification of the parallel artificial membrane permeation assay (PAMPA) for the prediction of blood-brain barrier penetration (PAMPA-BBB). The assay was developed with 30 structurally diverse commercial drugs and validated with 14 Wyeth Research compounds. The PAMPA-BBB assay has the advantages of. predicting passive blood-brain barrier penetration with high success, high throughput, low cost, and reproducibility. (C) 2003 Editions scientitiques et medicales Elsevier SAS. All rights reserved.
引用
收藏
页码：223 / 232
页数：10
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