Effects of amphetamine and BMPEA and their respective analogs on release of [3H]MPP+ at the DAT and NET in rat brain synaptosomes
Data are mean ± S.D. for N = 3 experiments performed in triplicate. The % Emax value is defined as the percentage of maximal releasing response induced by 10 µM tyramine. DAT/NET ratio = (DAT IC50 −1)/(NET IC50 −1); higher values indicate greater DAT selectivity.
| Drug | Release at DAT EC50 [%Emax] | Release at NET EC50 [%Emax] | DAT/NET Ratio |
|---|---|---|---|
| nM | nM | ||
| Amphetamine | 5 ± 1 [104] | 9 ± 2 [95] | 1.80 |
| Methamphetamine | 7 ± 2 [108] | 16 ± 3 [97] | 2.29 |
| Dimethylamphetamine | 1250 ± 231 [78] | 223 ± 40 [84] | 0.18 |
| BMPEA | 627 ± 102 [101] | 126 ± 21 [94] | 0.20 |
| MPPA | 574 ± 52 [103] | 154 ± 25 [80] | 0.27 |
| DMPPA | Inactive | 1337 ± 354 [67] | — |