TABLE 1

MRP2-mediated ATP-dependent [3H]TUDC transport: effect of potential modulators

Data are expressed as clearance values (microliters per milligram per minute, mean ± S.D. of triplicate determinations) and were obtained in the absence or presence of potential modulators in the concentrations indicated. The concentration of [3H]TUDC was 300 nM. Values of ATP-dependent MRP2-mediated transport with a mean ± S.D. (signal/noise ratio) of <1.5 were considered nondetectable (N.D.).


Treatment

Clearance (Mean ± S.D.)
(μl / mg / min)
0.3 μM TUDC N.D.
    +1 μM LTC4 N.D.
    +3 mM MeSG N.D.
+100 μM MTX N.D.
+10 μM TLCS N.D.
+100 μM TUDC 4.7 ± 1.6*
+20 μM E217G 8.7 ± 2.3*
+50 μM E23G
14.4 ± 1.9*
  • LTC4, leukotriene C4; MTX, methotrexate; MeSG, S-methyl-glutathione; TLCS, taurolithocholate sulfate.

  • * Transport in MRP2-expressing membrane vesicles significantly different (P < 0.05) from that in control (EV) membrane vesicles.