Table 2. Summary of inhibitory activities in [3H]DA uptake assay in WT and mutated hDAT in the presence of DA, cocaine and GBR12909.
IC50 (nM) | WT hDAT | H547A | H547P | H547R | H547D | Y548H | Y551H |
---|---|---|---|---|---|---|---|
DA | 1720 ± 206 | 5356 ± 978* | 300 ± 48* | 2454 ± 366 | 1168 ± 154 | 1744 ± 105 | 663 ± 70* |
Cocaine | 294 ± 34 | 338 ± 26 | 238 ± 26 | 470 ± 33 | 198 ± 32 | 77 ± 9* | 59 ± 7* |
GBR12909 | 262 ± 42 | 270 ± 85 | 332 ± 13 | 98 ± 17 | 344 ± 18 | 162 ± 44 | 279 ± 46 |
Data are presented as mean ± S.E.M. values from five to seven independent experiments performed in duplicates. *p < 0.05 compared with WT hDAT (unpaired Student’s t test).