Table 1. Effects of Test Drugs on Transporter-Mediated Release from Rat Brain Synaptosomes.
| Test drug | [3H]MPP+ release via NET EC50 (nM) | [3H]MPP+ release via DAT EC50 (nM) | [3H]5-HT release via SERT EC50 (nM) | NET/DAT ratio | DAT/SERT ratio |
|---|---|---|---|---|---|
| Mephedrone | 62.7±17.1 | 49.1±8.32 | 118.3±25.9 | 0.78 | 2.41 |
| Methylone | 152.3±33.2 | 133.0±11.2 | 242.1±48.3 | 0.87 | 1.82 |
| MDMA | 54.1±8.9 | 51.2±6.3 | 49.6±5.4 | 0.95 | 0.97 |
| Methamphetamine | 13.8±3.1 | 8.5±1.4 | 1291.7±241.6 | 0.62 | 152.0 |
Data are mean±SD for N=6 (NET) or N=3 (DAT and SERT) separate experiments. NET/DAT ratio=1/(NET EC50) divided by 1/(DAT EC50) for each drug; higher value indicates greater NET selectivity. DAT/SERT ratio=1/(DAT EC50) divided by 1/(SERT EC50) for each drug; higher value indicates greater DAT selectivity.