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Interactions between riluzole and ABCG2/BCRP transporter

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dc.contributor.author Milane, Aline
dc.contributor.author Vautier, Sarah
dc.contributor.author Chacun, Helene
dc.contributor.author Meininger, Vincent
dc.contributor.author Bensimon, Gilbert
dc.contributor.author Farinotti, Robert
dc.contributor.author Fernandez, Christine
dc.date.accessioned 2016-10-04T09:51:02Z
dc.date.available 2016-10-04T09:51:02Z
dc.date.copyright 2009 en_US
dc.identifier.issn 0304-3940 en_US
dc.identifier.uri http://hdl.handle.net/10725/4498
dc.description.abstract Amyotrophic lateral sclerosis (ALS) is a neurodegenerative fatal disease. Drugs used in this disease need to cross the blood–brain barrier (BBB). Only riluzole is approved for ALS treatment. We have investigated riluzole as a breast cancer resistance protein (BCRP) substrate by studying its brain transport in CF1 mdr1a (−/−) mice and its intracellular uptake on BeWo cells (human placental choriocarcinoma cell line). We have also investigated the effect of riluzole on BCRP expression level and on its activity using the prazocin as a test probe for brain transport and intracellular uptake. Assays on mdr1a (−/−) mice and BeWo cells showed a higher uptake of riluzole when pretreated with a BCRP inhibitor. After repeated doses of riluzole, BCRP activity was increased in CF1 mdr1a (−/−) mice, riluzole uptake was decrease and both BCRP expression and activity were increased in BeWo cells. In conclusion, we report in this study that riluzole is transported by BCRP at the BBB level and can enhance its function. These results taken with our previous studies on riluzole and P-glycoprotein show that drug–drug interactions between riluzole and efflux transporters substrates may occur at the BBB level and should be taken into account in future clinical trial design in ALS. en_US
dc.language.iso en en_US
dc.title Interactions between riluzole and ABCG2/BCRP transporter en_US
dc.type Article en_US
dc.description.version Published en_US
dc.author.school SOP en_US
dc.author.idnumber 200904164 en_US
dc.author.department N/A en_US
dc.description.embargo N/A en_US
dc.relation.journal Neuroscience Letters en_US
dc.journal.volume 452 en_US
dc.journal.issue 1 en_US
dc.article.pages 12-16 en_US
dc.keywords BCRP en_US
dc.keywords Riluzole en_US
dc.keywords Amyotrophic lateral sclerosis en_US
dc.keywords Blood–brain barrier en_US
dc.keywords CF1 mdr1a (−/−) mice en_US
dc.keywords BeWo cells en_US
dc.identifier.doi http://dx.doi.org/10.1016/j.neulet.2008.12.061 en_US
dc.identifier.ctation Milane, A., Vautier, S., Chacun, H., Meininger, V., Bensimon, G., Farinotti, R., & Fernandez, C. (2009). Interactions between riluzole and ABCG2/BCRP transporter. Neuroscience letters, 452(1), 12-16. en_US
dc.author.email aline.milane@lau.edu.lb en_US
dc.identifier.tou http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php en_US
dc.identifier.url http://www.sciencedirect.com/science/article/pii/S0304394009000020 en_US


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