TABLE 1

Kinetic parameters of the uptake of anionic compounds and nucleoside derivatives by kidney slices, rOat1- and rOat3-expressing LLC-PK1 cells

Data shown in Figs. 2, 3, 5, 6, and 9 were used to determine the Vmax, Km, and Ki values for the uptake of organic anions by cDNA-transfected cells and kidney slices. PAH and pravastatin were used as substrate to determine the Ki values for the rOat1- and rOat3-expressing cells, respectively. Each value represents the mean ± S.D. (n = 3)



rOat1-LLC

rOat3-LLC

Kidney Slice

Km or Ki
Vmax
Vmax/Km
Km or Ki
Vmax
Vmax/Km
Km or Ki
Vmax
Vmax/Km
μM pmol/min/mg protein μl/min/mg protein μM pmol/min/mg protein μl/min/mg protein μM nmol/min/g kidney ml/min/g kidney
Temocaprilat 0.556 ± 0.376* 3.71 ± 0.85 6.67 1.41 ± 0.97* 3.71 ± 0.85 3.61 0.22 ± 0.18* 0.11 ± 0.03 0.500
305 ± 23* 85.3 ± 4.9 0.280
2.4-D 10.2 ± 1.2* 1270 ± 98 125 12.3 ± 3.4 26.3 ± 10.4* 16.2 ± 6.5 0.616
AZT 41.5 ± 9.9* 329 ± 63 7.93 143 ± 34 20% inhibition at 3 mM
Estrone sulfate 50.1 ± 23.4 5.32 ± 1.2* 39.6 ± 5.9 7.44 0.82 ± 0.72* 0.52 ± 0.37 0.634
125 ± 39* 73.5 ± 19.5 0.588
ACV 981 ± 217 1460 ± 256 40% inhibition at 3 mM
DHEAS 80.9 ± 29.0 12.3 ± 1.4* 132 ± 10 10.7 9.59 ± 4.86* 6.24 ± 2.69 0.651
PCG 973 ± 134 85.1 ± 9.2* 243 ± 24 2.86 118 ± 38* 24.2 ± 6.4 0.205
Salicylate 551 ± 100 511 ± 167 2.81 ± 1.87* 1.66 ± 0.74 0.591







550* (fixed)
50.1 ± 10.6
0.091
  • * Km value