Table 3.
Binding inhibition of [3H]-CFT to adherent HEK 293 cells expressing human and rat MATs.
| Cocaine | MDPV | d-Amphetamine | MDMA | Fenfluramine | Mephedrone | |
|---|---|---|---|---|---|---|
| IC50 ± SD (µM) | ||||||
| Cell line 1 | ||||||
| hSERT | 0.25 ± 0.03 | 1.4 ± 0.3 | 57.5 ± 11.2 | 4.9 ± 0.9 | 1.8 ± 0.8 | 5.0 ± 1.0 |
| hDAT | 0.24 ± 0.09 | 0.014 ± 0.002 | 5.2 ± 3.6 | 34.8 ± 6.2 | 24.7 ± 5.9 | 3.4 ± 0.4 |
| hNET | 0.16 ± 0.04 | 0.027 ± 0.005 | 0.6 ± 0.1 | 4.4 ± 0.8 | 4.4 ± 0.3 | 0.8 ± 0.1 |
| Cell line 2 | ||||||
| hSERT | 1.9 ± 0.4 | 3.6 ± 0.6 | 25.6 ± 5.3 | 8.1 ± 1.6 | 1.15 ± 0.02 | 4.9 ± 1.2 |
| hDAT | 0.23 ± 0.03 | 0.03 ± 0.01 | 9.9 ± 2.6 | 33.0 ± 9.6 | 24.2 ± 2.4 | 3.4 ± 0.6 |
| hNET | 0.18 ± 0.02 | 0.03 ± 0.01 | 0.2 ± 0.1 | 1.8 ± 0.7 | 3.2 ± 1.8 | 0.4 ± 0.1 |
| Cell line 3 | ||||||
| rSERT | 0.17 ± 0.03 | 1.3 ± 0.6 | 22.5 ± 5.8 | 2.8 ± 0.4 | 2.8 ± 0.1 | 2.4 ± 0.7 |
| rDAT | 0.31 ± 0.09 | 0.02 ± 0.01 | 7.0 ± 2.9 | 28.4 ± 8.9 | 29.6 ± 7.7 | 5.6 ± 1.1 |
| rNET | 0.3 ± 0.2 | 0.03 ± 0.01 | 0.04 ± 0.02 | 0.4 ± 0.2 | 1.5 ± 0.5 | 0.2 ± 0.1 |
[3H]-CFT binding assays were conducted as described in Radioligand Uptake and Binding in Adherent Transporter-Transfected HEK Cells. IC50 values represent means ± SD of at least three independent experiments.