Table 5.
Radioligand uptake inhibition in rat synaptosomes and HEK 293 cell lines stably expressing rat MATs.
| Cocaine | MDPV | d-Amphetamine | MDMA | Fenfluramine | Mephedrone | |
|---|---|---|---|---|---|---|
| IC50 ± SD (µM) | ||||||
| SERT | ||||||
| Synaptosome | 0.31 ± 0.17 1 | 3.3 ± 0.3 1 | 3.4 ± 0.3 1 | 0.24 ± 0.01 2 | 0.27 ± 0.07 2 | 0.42 ± 0.03 1 |
| Cell | 4.3 ± 2.1 | 31.6 ± 7.6 | 103.5 ± 21.5 | 13.8 ± 4.7 | 12.7 ± 2.8 | 13.1 ± 3.3 |
| DAT | ||||||
| Synaptosome | 0.21 ± 0.02 1 | 0.004 ± 0.001 1 | 0.09 ± 0.02 1 | 1.6 ± 0.6 2 | 23.7 ± 1.3 2 | 0.8 ± 0.1 1 |
| Cell | 2.2 ± 1.6 | 0.04 ± 0.03 | 2.3 ± 1.3 | 24.8 ± 10.8 | 140.5 ± 14.2 | 12.0 ± 3.4 |
| NET | ||||||
| Synaptosome | 0.29 ± 0.03 1 | 0.026 ± 0.008 1 | 0.07 ± 0.02 1 | 0.5 ± 0.2 2 | 1.9 ± 0.2 2 | 0.49 ± 0.07 1 |
| Cell | 2.4 ± 2.0 | 0.07 ± 0.02 | 0.13 ± 0.03 | 0.9 ± 0.3 | 6.0 ± 2.2 | 0.3 ± 0.2 |
1
Value reported previously (Baumann et al., 2013)
2
Value reported previously (Rothman et al., 2003)
3
[3H]-substrate uptake inhibition assays were conducted as described in Method 1: Uptake Inhibition in Adherent Transporter-Transfected HEK Cells. IC50 values represent means ± SD of at least three independent experiments.