Ki | |||
---|---|---|---|
DBSP | E3040 glucuronide | E3040 sulfate | |
μM | |||
E3040 glucuronide uptake | 8.38 ± 1.24 | – | 6.29 ± 0.99 |
E3040 sulfate uptake | 5.41 ± 0.47 | 66.3 ± 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.