Transport of xanthurenic acid by rat/human organic anion transporters OAT1 and OAT3.

Kynurenic acid, a tryptophan metabolite, is involved in psychiatric disease. Our laboratory previously described its transport by rat/human organic anion transporters rOAT1, hOAT1, rOAT3 and hOAT3, which are involved in drug disposition. In this study, we performed an uptake experiment using Xenopus laevis oocytes to examine the transport of xanthurenic acid, a tryptophan catabolite and kynurenic acid analog, by various transporters. All the transporters tested stimulated the uptake of xanthurenic acid into oocytes. The transport activity of xanthurenic acid by hOAT1 was greater than that by rOAT1. In OAT3, the rat homolog showed efficient transport, compared with hOAT3. The apparent values of Km and Vmax for the transport by hOAT1 were 4.83 µM and 26.0 pmol/oocyte/h respectively. In rOAT3, the respective values were 6.87 µM and 21.7 pmol/oocyte/h. This is the first report on xanthurenic acid transport by OAT1 and OAT3.