(a)Effect of PKA activator Bt2-cAMP on hOAT3 transport activity. hOAT3-expressing cells were treated with Bt2-cAMP at various doses for 30 min. 4-min uptake of [3H]-estrone sulfate (ES, 0.3 μM) was then determined. Transport activity was expressed as % of the uptake in control cells (mock cells). The data correspond to the uptake into hOAT3-expressing cells minus uptake into mock cells and was normalized to protein concentration. Values are mean ± S.D. (n = 3). *P<0.05. (b) Selectivity of PKA on hOAT3 transport activity. hOAT3-expressing cells were pretreated with or without a PKA inhibitor H-89 (4μM, 10min). After that, the cells were treated with PKA activator Bt2-cAMP (10μM, 30min) with or without PKA inhibitor H-89 (4μM, 30min), or H-89 alone, followed by measuring the uptake of [3H] estrone sulfate (ES, 4min, 0.3 μM). Transport activity was expressed as % of the uptake in control cells. The data correspond to the uptake into hOAT3-expressing cells minus uptake into mock cells and was normalized to protein concentration. Values are mean ± S.D. (n = 3). *P<0.05.