rOCT1 | TEA+ App. Km | MPP+ App. Km | TEA+ IC50 | TBuA+ IC50 | |
---|---|---|---|---|---|
µM | |||||
I: HEK 1-s uptake | WT | 62 ± 7.6 (4) | 3.9 ± 0.5 (4) | 42 ± 7.1 (4) | 0.97 0.22 (4) |
II: HEK 2-min uptake | WT | 384 ± 120 (3)*** | 78 ± 9.8 (3)*** | 639 ± 40 (3)*** | 8.0 ± 1.8 (3)*** |
III: Ooc. 30-min uptake | WT | 75 ± 11 (8)### | 4.9 ± 1.4 (4)### | 132 ± 21 (6)***,### | 8.2 ± 1.8 (3)*** |
I: HEK 1-s uptake | Y222F | 59 ± 15 (4) | 5.1 ± 1.7 (3) | 20 ± 1.5 (3) | 0.28 ± 0.06 (3) |
II: HEK 2-min uptake | Y222F | 87 ± 16 (3)*** | 526 ± 132 (3)*** | 0.70 ± 0.08 (3)••• | |
III: Ooc. 30-min uptake | Y222F | 21 ± 1.5 (4)••• | 9.0 ± 0.7 (3)•,### | 54 ± 9.4 (3)••,### | 6.0 ± 1.1 (3)***,### |
I: HEK 5-s uptake | D475E | 18 ± 5.0 (4) | 4.8 ± 0.9 (4) | 53 ± 8.1 (4) | 0.49 ± 0.10 (3) |
II: HEK 2-min uptake | D475E | 21 ± 2.1 (3)*** | 81 ± 17 (3)* | 0.50 ± 0.08 (3) | |
III: Ooc. 30-min uptake | D475E | 18 ± 1.0 (3) | 3.1 ± 0.9 (3)### | 8.1 ± 1.2 (3)**,### | 0.32 ± 0.15 (3) |
App., apparent; Ooc., oocytes; WT, wild-type.
↵* P < 0.05;
↵** P < 0.01;
↵*** P < 0.001 difference to experimental condition I measured by ANOVA and post hoc Tukey test;
↵• P < 0.05;
↵•• P < 0.01;
↵••• P < 0.001 difference to experimental condition I measured by Student’s t test;
# P < 0.05;
## P < 0.01;
↵### P < 0.001 difference to experimental condition II measured by ANOVA and post hoc Tukey test.