High throughput artificial membrane permeability assay for blood-brain barrier
High throughput artificial membrane permeability assay for blood-brain barrier
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DOI：
10.1016/s0223-5234(03)00012-6
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发表时间：
2003-03-01
影响因子：
6.7
通讯作者：
Carter, GT
中科院分区：
文献类型：
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作者：
Di, L;Kerns, EH;Carter, GT
最近在高通量生物活性筛选和组合化学方面的进展极大地扩大了候选药物的数量。在药物发现计划的早期快速筛选血脑屏障穿透潜力为化合物的选择和指导合成以获得所需的中枢神经系统特性提供了重要信息。在本文中，我们讨论了一种改进的平行人工膜渗透试验(PAMPA)用于预测血脑屏障通透性(PAMPA-BBB)。该分析是用30种结构不同的商业药物开发的，并用14种惠氏研究化合物进行了验证。PAMPA-BBB检测方法具有以下优点。预测被动血脑屏障穿透具有高成功率、高通量、低成本和重复性。(C)2003年版《爱思唯尔科学与医学》。版权所有。
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.