ArticleEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences2009
P-glycoprotein deficient mouse in situ blood-brain barrier permeability and its prediction using an in combo PAMPA model.
Article in European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 74 citations in OpenAlex.
- Brain endothelial permeability, transport, and flow assessed over 10 orders of magnitude using the in situ brain perfusion technique.Fluids and barriers of the CNS · 2024Article
- Evaluation of the Ability of PAMPA Membranes to Emulate Biological Processes through the Abraham Solvation Parameter Model.Membranes · 2023Article
- Intracellular Binding of Terfenadine Competes with Its Access to Pancreatic ß-cell ATP-Sensitive KThe Journal of membrane biology · 2023Article
- Development of artificial neural network models to predict the PAMPA effective permeability of new, orally administered drugs active against the coronavirus SARS-CoV-2.Network modeling and analysis in health informatics and bioinformatics · 2023Article
- Article
- Development of an a priori computational approach for brain uptake of compounds in an insect model system.Bioorganic & medicinal chemistry letters · 2021Article
- Lost in modelling and simulation?ADMET & DMPK · 2021Article
- Oxidative stress-induced activation of Abl and Src kinases rapidly induces P-glycoprotein internalization via phosphorylation of caveolin-1 on tyrosine-14, decreasing cortisol efflux at the blood-brain barrier.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2020Article
- Improved Prediction of Blood-Brain Barrier Permeability Through Machine Learning with Combined Use of Molecular Property-Based Descriptors and Fingerprints.The AAPS journal · 2018Article
- Article
- Molecular determinants of blood-brain barrier permeation.Therapeutic delivery · 2015Review
- Article
- Challenges of using in vitro data for modeling P-glycoprotein efflux in the blood-brain barrier.Pharmaceutical research · 2014Review
- In vitro, in vivo and in silico models of drug distribution into the brain.Journal of pharmacokinetics and pharmacodynamics · 2013Review
- Blood-brain barrier structure and function and the challenges for CNS drug delivery.Journal of inherited metabolic disease · 2013Review
- Predicting efflux ratios and blood-brain barrier penetration from chemical structure: combining passive permeability with active efflux by P-glycoprotein.ACS chemical neuroscience · 2013Article
- Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries.The Journal of organic chemistry · 2012Article
- Computational prediction of blood-brain barrier permeability using decision tree induction.Molecules (Basel, Switzerland) · 2012Article
- In vitro blood-brain barrier models: current and perspective technologies.Journal of pharmaceutical sciences · 2012Review
- Biorelevant pK(a) (37 °C) predicted from the 2D structure of the molecule and its pK(a) at 25 °C.Journal of pharmaceutical and biomedical analysis · 2011Article
Corrections and comments
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Authors and funding
5 authors at 4 institutions in 2 countries.
Funding
Abstract
The purpose of the study was to assess the permeability of mouse blood-brain barrier (BBB) to a diverse set of compounds in the absence of P-glycoprotein (Pgp) mediated efflux, to predict it using an in combo PAMPA model, and to explore its role in brain penetration classification (BPC). The initial brain uptake (K(in)) of 19 compounds in both wild-type and Pgp mutant [mdr1a(-/-)] CF-1 mice was determined by the in situ brain perfusion technique. PAMPA measurements were performed, and the values were used to develop an in combo model, including Abraham descriptors. Published rodent K(in) values were used to enhance the dataset and validate the model. The model predicted 92% of the variance of the training set permeability. In all, 182 K(in) values were considered in this study, spanning four log orders of magnitude and where Pgp decreased brain uptake by as much as 14-fold. The calculated permeability-surface area (PS) values along with literature reported brain tissue binding were used to group molecules in terms of their brain penetration classification. The in situ BBB permeability can be predicted by the in combo PAMPA model to a satisfactory degree, and can be used as a lower-cost, high throughput first-pass screening method for BBB passive permeability.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.