TABLE 1

OATP-B-mediated uptake of various anionic compounds Uptake of each compound into HEK/OATP-B cells and HEK/Mock cells was measured for 10 min at 37°C and pH 7.4. The concentration of each compound is shown in parentheses. Each value represents the mean ± S.E.M. of four experiments. OATP-B-mediated uptake was obtained by subtracting the uptake into HEK/Mock cells from that into HEK/OATP-B cells. The significance of differences between the uptake into HEK/Mock cells and that into HEK/OATP-B cells was determined by applying Student's t test.


Anionic Compound (Concentration)

Uptake

p Value
HEK/Mock
HEK/OATP-B
OATP-B-Mediated
μl/mg protein/10 min
[3H]Estrone-3-sulfate (12.8 nM) 6.45 ± 0.19 211 ± 3 204 <0.001
[3H]DHEAS (17.4 nM) 5.92 ± 0.25 12.7 ± 0.6 6.8 <0.001
[3H]Taurocholic acid (41.9 nM) 2.55 ± 0.14 2.95 ± 0.35 0.40 N.S.
[14C]Salicylic acid (1.43 μM) 9.52 ± 0.76 11.2 ± 0.2 1.7 N.S.
[14C]Ibuprofen (11.3 μM) 12.6 ± 0.5 12.4 ± 0.2 –0.2 N.S.
[3H]Glibenclamide (10.1 nM) 82.0 ± 4.3 135 ± 1 53 <0.001
[14C]Tolbutamide (8.82 μM)
7.25 ± 0.19
7.50 ± 0.39
0.25
N.S.
  • DHEAS, dehydroepiandrosterone sulfate; N.S., not statistically significant.