TABLE 1

Inhibitory effects of various compounds on the uptake of [3H]estrone-3-sulfate by OATP-B expressed in HEK293 cells

OATP-B cDNA- or mock-transfected cells were preincubated for 20 min at 37°C in the uptake buffer (pH 7.4). Uptake of [3H]estrone-3-sulfate (4.76 nM) was measured for 10 min at 37°C by incubating the cells in the uptake buffer (pH 5.5), and the results are shown as percentage of control uptake measured in the absence of inhibitor after correcting for the uptake by mock-transfected cells. Each value represents the mean and S.E.M. (n = 3 or 4).


Inhibitor

Concentration

Relative Uptake
mM % of control
Pravastatin 10 32.5 ± 3.0*
Acetic Acid 10 86.1 ± 3.1
Lactic Acid 10 85.6 ± 2.9
Benzoic Acid 10 56.1 ± 3.5*
Nicotinic Acid 10 59.7 ± 2.9*
Oxalic Acid 10 83.9 ± 1.9
Phthalic Acid 10 42.7 ± 3.5*
Citric Acid 10 97.7 ± 2.2
DIDS
1
8.4 ± 1.3*
  • * Indicates a significant difference from the control (p < 0.05).