TABLE 3

IC50 values for high-affinity binding site and low-affinity binding site for inhibition of [3H]MPP+ uptake (0.0125, 0.125, or 5.0 μM) by 3TC in CHO-hOCT1 The statistical comparison between reference IC50 value ([MPP+] at 0.0125 μM) and the other two MPP+ concentrations was done (*, p < 0.05).


[MPP+] (μM)

CHO-hOCT1: IC50 Values of 3TC Two-Binding Sites
High-Affinity Binding Site
Low-Affinity Binding Site
pM mM
0.0125 12.3 ± 0.25 1.90 ± 0.14
0.125 145.5 ± 2.15* 1.12 ± 0.07
5.0
2127.5 ± 38.5*
1.42 ± 0.08
  • * p < 0.05, IC50 different from the reference one (0.0125 μM MPP+)