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dc.contributorFacultad de Veterinariaes_ES
dc.contributor.authorBlanco Paniagua, Esther 
dc.contributor.authorGarcia-Lino, Alba Maria
dc.contributor.authorGarcía Mateos, Dafne
dc.contributor.authorÁlvarez de Felipe, Ana Isabel 
dc.contributor.authorMerino Peláez, Gracia 
dc.contributor.otherFisiologiaes_ES
dc.date2021
dc.date.accessioned2021-12-21T23:21:24Z
dc.date.available2021-12-21T23:21:24Z
dc.identifier.issn0009-2797
dc.identifier.urihttp://hdl.handle.net/10612/13754
dc.descriptionP. 109537-109544es_ES
dc.description.abstractThe Breast Cancer Resistance Protein (BCRP/ABCG2) is an ATP-binding cassette efflux transporter that is expressed in the apical membrane of cells from relevant tissues involved in drug pharmacokinetics such as liver, intestine, kidney, testis, brain and mammary gland, among others. Tolfenamic acid is an anti-inflammatory drug used as an analgesic and antipyretic in humans and animals. Recently, tolfenamic acid has been repurposed as an antitumoral drug and for use in chronic human diseases such as Alzheimer. The aim of this work was to study whether tolfenamic acid is an in vitro Abcg2 substrate, and to investigate the potential role of Abcg2 in plasma exposure, secretion into milk and tissue accumulation of this drug. Using in vitro transepithelial assays with cells transduced with Abcg2, we showed that tolfenamic acid is an in vitro substrate of Abcg2. The in vivo effect of this transporter was tested using wild-type and Abcg2− /− mice, showing that after oral and intravenous administration of tolfenamic acid, its area under the plasma concentration-time curve in Abcg2− /− mice was between 1.7 and 1.8-fold higher compared to wild-type mice. Abcg2− /− mice also showed higher liver and testis accumulation of tolfenamic acid after intravenous administration. In this study, we demonstrate that tolfenamic acid is transported in vitro by Abcg2 and that its plasma levels as well as its tissue distribution are affected by Abcg2, with potential pharmacological and toxicological consequences.es_ES
dc.languageenges_ES
dc.publisherElsevieres_ES
dc.subjectFisiologíaes_ES
dc.subject.otherABCG2es_ES
dc.subject.otherTolfenamic acides_ES
dc.subject.otherTransportes_ES
dc.subject.otherPlasma levelses_ES
dc.subject.otherTissue distributiones_ES
dc.titleRole of the Abcg2 transporter in plasma levels and tissue accumulation of the anti-inflammatory tolfenamic acid in micees_ES
dc.typeinfo:eu-repo/semantics/articlees_ES
dc.identifier.doi10.1016/j.cbi.2021.109537
dc.description.peerreviewedSIes_ES
dc.rights.accessRightsinfo:eu-repo/semantics/openAccesses_ES
dc.journal.titleChemico-Biological Interactionses_ES
dc.volume.number345es_ES
dc.page.initial109537es_ES
dc.page.final109544es_ES
dc.type.hasVersioninfo:eu-repo/semantics/publishedVersiones_ES


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