Cited by 1,195Barrier Structure and Function StudiesDrug Transport and Resistance MechanismsComputational Drug Discovery Methods

High throughput artificial membrane permeability assay for blood–brain barrier

Di, Li, Kerns, Edward H, Fan, Kristi, McConnell, Oliver J, Carter, Guy T·2003·European Journal of Medicinal Chemistry

Abstract

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.

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Crossref · 10.1016/s0223-5234(03)00012-6

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Authors
Di, L., Kerns, E. H., Fan, K., McConnell, O. J., & Carter, G. T.
Affiliations
Wyeth (US)
Corresponding author
Di, Li
Venue
European Journal of Medicinal Chemistry
Publisher
Elsevier BV
Published
2003-03
Volume
38
Issue
3
Pages
223-232
ISSN
0223-5234 (ISSN-L)
OpenAlex
W2026976753
Cited by
1,195
References
0
Citations by year
2026: 71 · 2025: 91 · 2024: 88 · 2023: 71 · 2022: 96 · 2021: 92 · 2020: 83 · 2019: 71 · 2018: 81 · 2017: 70 · 2016: 79 · 2015: 53 · 2014: 37 · 2013: 38 · 2012: 38
FWCI
7.78
Type
journal article
Language
en
Open access
closed
Locations
  • European Journal of Medicinal Chemistry (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
  • Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
  • Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
Keywords
blood-brain barrier penetration, high-throughput screening, CNS drug candidates, passive permeability, drug discovery
MeSH terms
Animals, Blood-Brain Barrier, Brain Chemistry, Cell Membrane Permeability, Drug Evaluation, Preclinical, Pharmaceutical Preparations, Lipids, Membranes, Artificial, Predictive Value of Tests, Robotics, Spectrophotometry, Ultraviolet, Swine, Reproducibility of Results, Combinatorial Chemistry Techniques, In Vitro Techniques

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