Table 1.
Apparent potency values of dopamine (pEC50) and inhibitory potency values of DAT inhibitors (pIC50) on U2OS-mock, U2OS-DAT or JumpIn-DAT (± dox) cells in TRACT experiments using a non-linear regression analysis model with a fixed pseudo-Hill slope of 1. Values are reported as the mean ± SEM of three to nine individual experiments performed in duplicate (n indicates the number of biological replicates). Significant difference between two mean potency values was determined by unpaired two-tailed Student’s t-test. *p < 0.05 (compared to U2OS-mock); ##p < 0.01 (compared to U2OS-DAT/dopamine); †††p < 0.001 (compared to JumpIn-DAT (−dox)). Comparison of multiple mean values to vehicle control was done using a one-way ANOVA with Dunnett’s post-hoc test. ‡‡‡p < 0.001 (compared to JumpIn-DAT (+dox)/dopamine). &&&p < 0.001 (compared to JumpIn-DAT (−dox)).
| Cell line | Compound | pEC50 ± SEM (EC50 in µM) |
pIC50 ± SEM (IC50 in µM) |
n |
|---|---|---|---|---|
| U2OS-mock | Dopamine | 5.3 ± 0.2 (5) | – | 3 |
| U2OS-DAT | Dopamine | 4.0 ± 0.2* (96) | – | 6 |
| Dopamine + 10 µM GBR12909 | 5.2 ± 0.2## (6) | – | 4 | |
| GBR12909 + 3.16 µM dopamine | – | 6.2 ± 0.1 (0.6) | 4 | |
| JumpIn-DAT –dox | Dopamine | 5.1 ± 0.1 (8) | – | 7 |
| JumpIn-DAT +dox | Dopamine | 4.3 ± 0.0††† (46) | – | 9 |
| Dopamine + 10 µM GBR12909 | 4.6 ± 0.2&&& (26) | – | 4 | |
| Dopamine + 10 µM cocaine | 4.9 ± 0.1‡‡‡ (13) | – | 4 | |
| GBR12909 + 10 µM dopamine | – | 6.6 ± 0.1 (0.2) | 4 | |
| Cocaine + 10 µM dopamine | – | 6.3 ± 0.2 (0.6) | 4 |