Table 1.
Monoamine uptake inhibition and transporter binding affinities at DAT and SERT of substituted cathinones and cocaine. For monoamine uptake inhibition assays, values are IC50, given as μM (mean ± SEM) and for transporter binding affinities assays, values are Ki, given as μM (mean ± SEM) of 6 independent experiments performed per triplicate. hDAT/hSERT inhibition and affinity ratios were also calculated, as mentioned in Section 4.
| Transfected HEK293 Cells | ||||||
|---|---|---|---|---|---|---|
| Monoamine Uptake Inhibition | Transporter Binding Affinities | |||||
| Compound | [3H]MPP+ Uptake at hDAT | [3H]5-HT Uptake at hSERT | hDAT/hSERT Inhibition Ratio | [3H]WIN35,428 Binding at hDAT | [3H]Imipramine Binding at hSERT | hDAT/hSERT Affinity Ratio |
| α-PVP | 0.129 (±0.002) | >100 | 3418 | 0.017 (±0.001) | >100 | 8514 |
| 3-F-α-PVP | 0.132 (±0.016) | >100 | 1819 | 0.014 (±0.001) | 63.53 (±7.62) | 4540 |
| 4-F-α-PVP | 0.154 (±0.019) | >100 | 1366 | 0.049 (±0.004) | 57.88 (±4.27) | 1173 |
| 3-Cl-α-PVP | 0.349 (±0.033) | 33.33 (±2.46) | 95 | 0.013 (± 0.001) | 16.43 (±0.50) | 1234 |
| 4-Cl-α-PVP | 0.391 (±0.025) | 15.17 (±0.24) | 38 | 0.016 (± 0.001) | 7.90 (±0.18) | 478 |
| 3,4-Cl-α-PVP | 0.266 (±0.012) | 12.74 (±0.28) | 47 | 0.011 (± 0.001) | 4.99 (±0.27) | 462 |
| 3-Br-α-PVP | 0.117 (±0.016) | 39.96 (±6.38) | 341 | 0.012 (±0.002) | 5.60 (±0.31) | 470 |
| 4-Br-α-PVP | 0.156 (±0.012) | 23.11 (±2.27) | 148 | 0.024 (±0.001) | 1.25 (±0.09) | 52 |
| Cocaine | 0.231 (±0.013) | 1.85 (±0.28) | 7.98 | 0.283 (±0.04) | 0.54 (±0.03) | 1.92 |
hDAT/hSERT ratio = 1/DAT IC50:1/SERT IC50.