Table 4.
Potency and efficacy of substituted phenethylamines and other compounds to release preloaded [3H]neurotransmitter from HEK-hDAT, HEK-hSERT and HEK-hNET cells.
| Drug | Drug-induced release of [3H]neurotransmitter | ||
|---|---|---|---|
| EC50 mean ± sem (μM) (n) | |||
| % maximum release ± sem* | |||
| hDAT [3H]DA | hSERT [3H]5-HT | hNET [3H]NE | |
| 25D-NBOMe | >100 μM (2) | >100 μM (2) | >33 μM (3) |
| 0.75 ± 0.48% | 0.59 ± 0.24% | 14.3 ± 8.5% | |
| 25E-NBOMe | >85 μM (3) | >100 μM (2) | >66 μM (3) |
| 5.8 ± 6.4% | 0.21 ± 0.77% | 17.1 ± 5.9% | |
| 25H-NBOMe | >100 μM (2) | >100 μM (2) | >66 μM (3) |
| −0.18 ± 0.26% | −0.27 ± 0.49% | 21 ± 12% | |
| 25I-NBOH | >100 μM (2) | >100 μM (2) | >100 μM (2) |
| −0.56 ± 0.35% | −0.27 ± 0.40% | 16 ± 16% | |
| 25N-NBOMe | >100 μM (2) | >100 μM (2) | >38 μM (3) |
| −0.89 ± 0.91% | −0.25 ± 0.54% | 25 ± 15% | |
| LSD | >54 μM (4) | >100 μM (2) | >91 μM (3) |
| 7.4 ± 4.7% | −0.59 ± 0.55% | 35.7 ± 4.2% | |
| DOM | >100 μM (2) | >100 μM (2) | >42 μM (4) |
| −0.20 ± 0.16% | 2.9 ± 3.4% | 25.5 ± 2.0% | |
| METH | 0.43 ± 0.15 (5) | 27.5 ± 7.0 (4) | 0.152 ± 0.056 (3) |
| 104.1 ± 1.3 | 104.9 ± 6.8% | 106.7 ± 3.3% | |
(n) Number of independent experiments.
*
Maximum release is defined as the maximum release (maximal AUC) induced by METH (1–10 μM, hDAT; 0.3–1 mM, hSERT; 0.3–1 μM, hNET) for each experiment.