IC50 values of methamphetamine, amphetamine, and p-OHMA for hOCT1–3 and hMATE1/2-K determined by one-binding site fitting
Results represent mean ± S.D. of three independent experiments each run in triplicate.
| Transporter | One-Binding Site | |||||
|---|---|---|---|---|---|---|
| Methamphetamine | Amphetamine | p-OHMA | ||||
| IC50 | Hill Slope | IC50 | Hill Slope | IC50 | Hill Slope | |
| μM | μM | μM | ||||
| hOCT1 | 21.1 ± 8.8 | 0.55 ± 0.02 | 96.7 ± 37 | 0.61 ± 0.28 | 12.0 ± 3.4 | 1.17 ± 0.14 |
| hOCT2 | 15.0 ± 6.8 | 0.56 ± 0.07 | 20.3 ± 16.9 | 0.44 ± 0.1 | 83.8 ± 22.3 | 1.55 ± 0.32 |
| hOCT3 | 300 ± 139 | 1.42 ± 0.68 | 363 ± 56.4 | 1.1 ± 0.2 | 44.4 ± 25.5 | 1.1 ± 0.26 |
| hMATE1 | 107 ± 38 | 0.79 ± 0.09 | 94.0 ± 25.3 | 0.89 ± 0.2 | 59.1 ± 14.3 | 0.84 ± 0.12 |
| hMATE2-K | 84.3 ± 12.9 | 1.63 ± 0.14 | 158 ± 48 | 1.9 ± 0.6 | 234 ± 86.8 | 1.21 ± 0.11 |