Table 5

K i values of DBSP and the conjugates for the uptake of E3040 glucuronide and sulfate

Ki
DBSPE3040 glucuronideE3040 sulfate
μM
E3040 glucuronide uptake8.38  ± 1.246.29  ± 0.99
E3040 sulfate uptake5.41  ± 0.4766.3  ± 9.8

The saturable uptake of [14C]E3040 conjugates in the presence and absence of inhibitors (fig. 8) was simultaneously fitted to equations 2 and 4 to determine the kinetic parameters. The uptake of [14C]E3040 glucuronide was described by one saturable (K m = 73.3 ± 15.3 μM;V max = 2.51 ± 0.49 nmol/min/106 cells) and one nonsaturable (P dif = 4.41 ± 0.74 μl/min/106 cells) components. The uptake of [14C]E3040 sulfate was described by one saturable (K m = 28.5 ± 2.7 μM; V max= 8.96 ± 0.66 nmol/min/106 cells) and one nonsaturable (P dif = 5.51 ± 1.75 μl/min/106cells) components. These K m, V maxand P dif values for E3040 conjugates were not significantly different from those reported in table 4.