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- W2682796510 abstract "<p class=ADMETabstracttext>The aim of this study was to assess the suitability of amiloride, rhodamine 6G and rhodamine 123 as non-radioactive substrates for characterizing hOCT2 using CHO cells. The uptake characteristics of these compounds were compared in wild-type (WT) and human organic cation transporter 2 (hOCT2)-stably transfected Chinese Hamster Ovary (CHO) cells. All the compounds were accumulated by the CHO-hOCT2 cells. Intracellular uptake of the compounds was higher in CHO cells stably-expressing hOCT2 compared to the WT. The uptake was concentration–dependent and saturable (except for rhodamine 123). The affinities of the compounds for the hOCT2 (in descending order) were: amiloride (K<sub>m</sub> = 72.63 ± 12.02 µM) > rhodamine 6 G (K<sub>m</sub> = 82.47 ± 29.15 µM). Uptake of amiloride in transfected cells was pH -dependent and significantly inhibited by hOCT2 inhibitors (quinine, verapamil and quinidine). Based on our kinetic data and other considerations, we recommend the use of amiloride for characterizing hOCT2 transporters.</p>" @default.
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- W2682796510 date "2017-06-22" @default.
- W2682796510 modified "2023-10-01" @default.
- W2682796510 title "Fluorescent organic cations for human OCT2 transporters screening: uptake in CHO cells stably expressing hOCT2" @default.
- W2682796510 doi "https://doi.org/10.5599/admet.5.2.389" @default.
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