TABLE 1

Effect of pHo on Oatp1a1-, OATP1B1-, and OATP1B3-mediated TCA, E217βG, and E3S uptake by transfected CHO cells

Stably transfected CHO cells were incubated in uptake medium (96 mM choline chloride, 5.3 mM KCl, 1.1 mM KH2PO4, 0.8 mM MgSO4, 1.8 mM CaCl2, 11 mM glucose, and 50 mM HEPES) containing the desired substrate (10 μM [3H]TCA, 10 μM [3H]E217βG, or 50 μM [3H]E3S) at 37°C for 15 min. Net uptake values are means ± S.D. from at least nine determinations per data point, obtained using cells from three different cultures.

Oatp1a1OATP1B1OATP1B3
pmol · mg protein1 · 15 min1
10 μM TCA
    pH 7.411 ± 238 ± 435 ± 3
    pH 6.522 ± 2a28 ± 5a55 ± 7a
10 μM E217βG
    pH 7.4274 ± 20203 ± 3763 ± 8
    pH 6.5393 ± 15a135 ± 17a132 ± 19a
50 μM E3S
    pH 7.41446 ± 71456 ± 51325 ± 35
    pH 6.52212 ± 187a573 ± 73479 ± 26a
  • a P < 0.05, on comparing pH 6.5 with pH 7.4 by paired t test.