Figure 10. Tranilast inhibits urate transport mediated by urate transporter OAT3 and OAT1. The uptake of [14C]‐urate (40 μmol/L) was performed in ND96 medium (pH 7.4) at ~25°C for 1 h. (A) The [14C]‐urate uptake by mouse OAT3 in oocytes remained unaffected if oocytes were preinjected with 50 nL of 100 mmol/L PZA but cis‐inhibited by 10 mmol/L PZA, nicotinate (Nico), or salicylate (Sal). The [14C]‐urate uptake by OAT3‐expressing oocytes was effectively inhibited by 50 μmol/L tranilast (Tran), 100 μmol/L benzbromarone (Benz) or 1.0 mmol/L probenecid (Prob). (B) The [14C]‐urate uptake by human OAT1 in oocytes was effectively inhibited by 100 μmol/L tranilast (Tran), 100 μmol/L benzbromarone (Benz) or 1.0 mmol/L probenecid (Prob). Data are mean ± S.E. with n = 12–15. *P < 0.001 compared with uptake in the presence of DMSO or in the absence of inhibitor. PZA, pyrazine carboxylate; Tran, Tranilast; Benz, Benzbromarone; Prob, probenecid; DMSO, dimethylsulfoxide.
Image published in: Mandal AK et al. (2017)
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