Table 4.
Substituted methcathinones and standard compounds: Affinity for the [3H]DHTB binding site and potency to inhibit [3H]5-HT uptake and stimulate release of [3H]NE at hVMAT2.
| Drug | Inhibition of [3H]DHTB binding Ki ± sem (µM)(n) |
Inhibition of [3H]5-HT uptake IC50 ± sem (µM)(n) |
Drug-induced release of [3H]NE EC50 ± sem (µM) (n) |
Release of [3H]NE % maximum release* ± sem or range** |
|---|---|---|---|---|
| Butylone | 730 ± 110(4) | 162 ± 55 (4) | 4.40 ± 0.52 (2) | 17.4 ± 1.1% |
| 4-FMC | >1 mM (2) | 178 ± 36 (6) | >100 µM (2) | 24.9 ± 5.7% |
| MDPV | 990 ± 270 (5) | >100 µM(3) | 148 ± 84 (5) | 35.8 ± 9.6% |
| Mephedrone | >1 mM (2) | 115.7 ± 8.8(5) | 66 ± 23 (3) | 33.1 ± 1.9% |
| Methylone | >1 mM (2) | >100 µM(3) | >100 µM (3) | 21.8 ± 8.5% |
| Naphyrone | 119 ± 20(5) | 21.4 ± 7.1 (3) | >100 µM (4) | 34 ± 14% |
| METH | 920 ± 110(11) | 4.72 ± 0.61 (5) | 79 ± 29(11) | 95.5 ± 2.1% |
| MDMA | 661 ± 58(3) | 5.8 ± 1.4 (3) | 114 ± 40(3) | 63 ± 13% |
| Methcathinone | >1 mM (3) | 117 ± 57(3) | 11.6 ± 7.3(3) | 42 ± 10% |
| Reserpine | 0.417 ± 0.061 (7) | 0.0066 ± 0.0013 (5) | ||
| RO4-1284 | 0.150 ± 0.015(8) | 0.098 ± 0.032 (5) |
(n) Number of independent experiments.
Hill slopes for [3H]DHTB binding ranged from −0.89 to −1.38.
*
Maximum release is defined as the maximum release (maximal AUC) induced by METH (100 µM or 1 mM).
**
The range is given when n=2.