ArticlePharmaceutical research2005
A fluorometric screening assay for drug efflux transporter activity in the blood-brain barrier.
Article in Pharmaceutical research, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- In Vitro Assessment of the Effect of Antiepileptic Drugs on Expression and Function of ABC Transporters and Their Interactions with ABCC2.Molecules (Basel, Switzerland) · 2017Article
- Nanoscale drug delivery systems and the blood-brain barrier.International journal of nanomedicine · 2014Review
- Quantitative fluorescence microscopy provides high resolution imaging of passive diffusion and P-gp mediated efflux at the in vivo blood-brain barrier.Journal of neuroscience methods · 2013Article
- Olomoucine II, but not purvalanol A, is transported by breast cancer resistance protein (ABCG2) and P-glycoprotein (ABCB1).PloS one · 2013Article
- Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry · 2012Article
- Radiosynthesis and in vivo evaluation of 1-[18F]fluoroelacridar as a positron emission tomography tracer for P-glycoprotein and breast cancer resistance protein.Bioorganic & medicinal chemistry · 2011Article
- Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein.Psychopharmacology · 2006Article
- Quantitative assessment of HIV-1 protease inhibitor interactions with drug efflux transporters in the blood-brain barrier.Pharmaceutical research · 2005Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
purposeTo examine the capability of a fluorometric assay to identify and characterize the drug efflux interactions of a broad spectrum of drug agents in an in vitro model of the blood-brain barrier (BBB).
methodsVarious concentrations of drug agent (1, 10, and 100 microM) were evaluated for their effect on the cellular accumulation of the P-glycoprotein (P-gp) probe R123 (3.2 microM), and the mixed P-gp and multidrug resistance-associated protein (MRP) probe, BCECF (1 microM), in bovine brain microvessel endothelial cell (BBMEC) monolayers. Drugs demonstrating a significant effect were further quantitated using an expanded concentration range and a nonlinear regression curve fit to determine the potency (IC50) and efficacy (Imax) of the drug for P-gp and/or MRP.
resultsSeveral of the 36 therapeutic agents examined showed drug efflux transporter interactions in BBMEC monlayers. Melphalan and risperidone significantly enhanced the accumulation of R123 over control (1.47- and 1.82-fold, respectively) with resulting IC50s of 1.4 and 14.6 microM, respectively. Chlorambucil and valproic acid significantly enhanced the accumulation of BCECF compared to control monolayers (2.02- and 4.01-fold, respectively) with resulting IC50s of 146.1 and 768.5 microM, respectively.
conclusionsThe current study demonstrates the feasibility of a fluorometric assay consisting of R123 and BCECF in assessing the drug efflux interactions of a variety of drugs in the BBB.
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