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dc.contributor.authorSALOMON, JOHANNAen
dc.contributor.authorEHRHARDT, CARSTENen
dc.contributor.authorBUCKLEY, STEPHENen
dc.date.accessioned2012-06-19T13:54:45Z
dc.date.available2012-06-19T13:54:45Z
dc.date.issued2012en
dc.date.submitted2012en
dc.identifier.citationJJ Salomon, S Endter, G Tachon, F Falson, ST Buckley, C Ehrhardt, Transport of the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (ASP+) in human respiratory epithelial cells, Eur J Pharm Biopharm, 81, 2, 2012, 351-359en
dc.identifier.otherYen
dc.identifier.urihttp://hdl.handle.net/2262/63819
dc.descriptionPUBLISHEDen
dc.description.abstractOrganic cation/carnitine transporters (OCT/N) mediate uptake of positively charged molecules. Their role in lung epithelium, however, is not well understood. OCT/N expression and activity was studied in cell lines of human alveolar (A549), bronchial (16HBE14o- and Calu-3) and intestinal (Caco-2) epithelium. Protein levels were largely comparable for all OCT/Ns in the respiratory epithelial cell lines studied, however, OCT2 was exclusively observed in A549 cells. OCT1 and -2 were present at significantly higher levels in Caco-2 cells, compared with the pulmonary epithelial cell types. OCTN1 and -2 were also more abundant in Caco-2. Only OCT3 was expressed evenly across all cell lines investigated. Uptake of 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (ASP+) was dependent on concentration, temperature, membrane potential and pH. In 16HBE14o-, Calu-3 and Caco-2 monolayers substrate saturation of ASP+ uptake was not reached. Alveolar A549 cells showed saturable ASP+ uptake via two transporter sites with Km values of 12.5?4.0 ?M and 456.9?164.5 ?M, respectively. This uptake was sensitive to organic cations, but insensitive to carnitine and lysine. We conclude that uptake of organic cations is facilitated by distinct pathways in different regions of lung mucosa. Luminally localised OCT2 appears to be exclusively involved in the alveolar epithelium, whereas basolateral localised OCT3 might play a role in alveolar as well as in bronchial epithelial cells.en
dc.description.sponsorshipThis work has been funded by a Strategic Research Cluster grant (07/SRC/B1154) under the National Development Plan co-funded by EU Structural Funds and SFI. STB was funded by an IRCSET Government of Ireland Postgraduate Scholarship in Science, Engineering and Technology. GT was the recipient of a bourse de mobilite internationale etudiante Explo'ra sup funded by the Region Rhone-Alpes.en
dc.format.extent351-359en
dc.language.isoenen
dc.relation.ispartofseriesEur J Pharm Biopharmen
dc.relation.ispartofseries81en
dc.relation.ispartofseries2en
dc.rightsYen
dc.subjectPharmacologyen
dc.subjectOrganic cation transportersen
dc.subjectBronchial epitheliumen
dc.subjectAlveolar epitheliumen
dc.subjectPulmonary drug dispositionen
dc.subjectInhalation biopharmaceuticsen
dc.titleTransport of the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (ASP+) in human respiratory epithelial cellsen
dc.typeJournal Articleen
dc.contributor.sponsorScience Foundation Ireland (SFI)en
dc.contributor.sponsorIrish Research Council for Science and Engineering Technology (IRCSET)en
dc.type.supercollectionscholarly_publicationsen
dc.type.supercollectionrefereed_publicationsen
dc.identifier.peoplefinderurlhttp://people.tcd.ie/ehrhardcen
dc.identifier.rssinternalid78525en
dc.identifier.doi10.1016/j.ejpb.2012.03.001en
dc.contributor.sponsorGrantNumber07/SRC/B1154en
dc.subject.TCDThemeImmunology, Inflammation & Infectionen
dc.identifier.rssurihttp://dx.doi.org/10.1016/j.ejpb.2012.03.001en
dc.identifier.orcid_id0000-0003-0730-1829en


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