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Figure 6. Functional characterization of human URAT1 as a nicotinate transporter; effects of uricosuric drugs. (A) Trans‐stimulatory effects of preloaded organic anions on [14C]‐nicotinate uptake by URAT1‐expressing oocytes: [14C]‐nicotinate transport rate via URAT1 was measured in URAT1‐expressing oocytes preloaded with 50 nL of 100 mmol/L Lac, PZA, PAH, BHB, or urate. *P < 0.001 compared with water‐injected control; NS, not significant. (B) Inhibition of [14C]‐nicotinate by URAT1 in the presence of extracellular urate or uricosuric drugs: The uptake of [14C]‐nicotinate (40 μmol/L) by URAT1‐expressing oocytes in exchange of preloaded intracellular PZA was determined after 1 h in the absence or presence of inhibitors (uricosuric drugs) that were added to the extracellular medium (pH 7.4) at the indicated concentrations. *P < 0.001 compared with DMSO/NaCl(ND96). Tran, Benz, Prob, DMSO. (C) The 50% inhibitory concentration (IC 50) curve of tranilast for [14C]‐nicotinate uptake by URAT1‐expressing oocytes preinjected with 50 nL of 100 mmol/L PZA 2 h before [14C]‐nicotinate uptake experiment. Data are mean ± S.E. with n = 12–15. BHB, β‐hydroxy butyrate; PAH, para‐aminohippurate; Lac, lactate, PZA, pyrazine carboxylate; PAHe , para‐aminohippurate; Tran, Tranilast; Benz, Benzbromarone. Image published in: Mandal AK et al. (2017) © 2017 The Authors. This image is reproduced with permission of the journal and the copyright holder. This is an open-access article distributed under the terms of the Creative Commons Attribution license Larger Image Printer Friendly View

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