TABLE 2

Comparison of in vitro inhibition constant of various drugs for OCT2- and MATE2-K–mediated uptake

Each value was determined from the data shown in Fig. 2. The equations for the calculations are described in Materials and Methods. Each value represents the mean ± computer-calculated S.D.

InhibitorhOCT2hMATE2-K
m1A 100 μMCreatinine 100 μMMetformin 10 μMm1A 100 μMCreatinine 100 μMMetformin 10 μM
Trimethoprim20 ± 526 ± 220 ± 22.4 ± 0.40.58 ± 0.110.92 ± 0.04
Pyrimethamine0.64 ± 0.180.93 ± 0.040.61 ± 0.040.22 ± 0.060.35 ± 0.050.22 ± 0.02
Cimetidine1.8 ± 0.436 ± 359 ± 1.45.3 ± 1.624 ± 55.2 ± 0.8