Table 1. Dopamine (DA) transporter uptake inhibition and substrate releasing effects of a series of phenethylamines as determined in rat brain synaptosomes.
| Name | Structure | DA UI IC50 (nM) | DA Release EC50 (nM) | Name | Structure | DA UI IC50 (nM) | DA Release EC50 (nM) |
|---|---|---|---|---|---|---|---|
| Phenethylamine |
|
39.5 ± 1.8 | PAL-27 |
|
208 ± 13 | ||
| Amphetamine |
|
8.7 ± 1.2 | Cathinone |
|
83.1 ± 9 | ||
| Methamphetamine |
|
24.5 ± 2.1 | Methcathinone |
|
49.9 ± 3.1 | ||
| PAL-99 |
|
88.5 ± 9.6 | PAL-434 |
|
46.8 ± 4.0 | ||
| PAL-426 |
|
225 ± 2.1 | Mephedrone |
|
49.1 ± 3.1 | ||
| PAL-503 |
|
271 ± 17 | Methylone |
|
133.0 ± 11 | ||
| PAL-505 |
|
2087 ± 195 | PAL-429 |
|
411 ± 98 | ||
| PAL-424 |
|
1013 ± 101 | N-Ethylpropion |
|
1014 ± 80a | ||
| PAL-550 |
|
2596 ± 408 | PAL-359 |
|
IA | ||
| PAL-90 |
|
IA | MDPV |
|
4.1 ± 0.06 | ||
| PAL-595 |
|
IA | Bupropion |
|
658 ± 178 |
Release EC50 and Uptake Inhibition IC50 values are reported as means ± SD and are the result of n= 3 performed in triplicate.
UI = Uptake Inhibition; IA = inactive with IC50 >10,000 nM. Cells are left blank where the major property of the compound is in the adjacent cell (releasing activity in top portion of table, or uptake inhibitory activity in the bottom portion).
From Yu et al., 2000.