TABLE 2

Inhibitory effect of various compounds on the uptake of [3H]digoxin and [3H]CCK-8 in SCHH lot Hu4165

The uptake of 0.05 μM [3H]digoxin or 1 μM [3H]CCK-8 was measured at 37°C for 5 min in the presence and absence of inhibitors. The CCK-8 control value was 1.06 pmol/mg protein/min. Data are expressed as a percentage of the control values ± S.D. (n = 3). Statistical significance was determined using the Student's t test as described under Materials and Methods.

InhibitorsConcentration[3H]Digoxin[3H]CCK-8
μM%Control%Control
Control (0.1% DMSO)a100 ± 3.1100 ± 10.4
Control (1% DMSO)b100 ± 7.0
Cyclosporine A1093.2 ± 9.216.0 ± 0.6*
BSP100113 ± 4.411.8 ± 2.0*
FCCP5063.8 ± 1.1*14.4 ± 0.3*
Rifampicin100120 ± 1.3*26.7 ± 3.3*
Digoxin10048.9 ± 1.3*29.0 ± 4.0*
Digoxin (1% DMSO)50055.5 ± 3.6*
  • DMSO, dimethyl sulfoxide.

  • * p < 0.01, significantly different from control.

  • a The digoxin control value was 0.18 pmol/(min · mg protein).

  • b The digoxin control value was 0.14 pmol/(min · mg protein).