TABLE 1

Uptake of different OCT2 substrates in HEK cells stably expressing wild-type OCT2 or the OCT2 p0.270Ala>Ser mutant protein

Each value represents the mean ± S.E.M. of n determinations from 2 to 3 independent experiments.



n

Km

Vmax

OCT2 Wild-Type
OCT2 p.270Ala>Ser
OCT2 Wild-Type
OCT2 p.270Ala>Ser
μM pmol/mg/min
MPP+ 6 19.5 ± 2.8 20.9 ± 4.3 579 ± 17 414 ± 18***
Dopamine 8 932 ± 77 1285 ± 132* 7559 ± 173 6820 ± 203*
Norepinephrine 12 5452 ± 498 5282 ± 907 2135 ± 90 1671 ± 132*
Metformin 7 3171 ± 401 3179 ± 390 10730 ± 582 10670 ± 561
Propranolol
6
11.8 ± 3.7
5.8 ± 3.6
201 ± 24
89 ± 17**
  • * p < 0.05; ** p < 0.01; *** p < 0.0001 vs. OCT wild-type.