Table 1.
Potency (EC50) and efficacy (%Emax) of psychoactive benzofuran compounds to release [3H]MPP+ via DAT and NET, or [3H]5-HT via SERT, in rat brain synaptosomes.
| Drug | DAT release EC50 (nM) [%Emax] | NET release EC50 (nM) [%Emax] | SERT release EC50 (nM) [%Emax] | DAT/SERT ratio | DAT/NET ratio |
|---|---|---|---|---|---|
| MDA | 106 ±7 [104%] | 47 ±7 [91%] | 162 ±28 [109%] | 1.53 | 0.43 |
| 5-APB | 31 ±3 [103%] | 21 ±4 [103%] | 19 ±2 [104%] | 0.61 | 0.67 |
| 6-APB | 10 ± 1 [101%] | 14 ±2 [98%] | 36 ±5 [100%] | 3.60 | 1.40 |
| MDMA | 120 ±8 [101%] | 90 ±13 [99%] | 85 ±16 [104%] | 0.71 | 0.75 |
| 5-MAPB | 41 ±3 [103%] | 24 ±3 [99%] | 64 ±7 [103%] | 1.56 | 0.58 |
| 6-MAPB | 20 ±2 [106%] | 14 ±2 [100%] | 33 ±4 [106%] | 1.65 | 0.70 |
Data are mean +/− SD for N=3 experiments performed in triplicate. Values in brackets are % of maximal release, as defined in Materials and Methods. DAT/SERT ratios are calculated as (DAT EC50)−1 /(SERT EC50)−1, where larger number indicates higher DAT selectivity. DAT/NET ratios are calculated as (DAT EC50)−1/(NET EC50)−1, where larger number indicates higher DAT selectivity.