Table 2.
Monoamine transport inhibition
| NET | DAT | SERT | DAT/SERT ratio | Recreational dose* mg | |
|---|---|---|---|---|---|
| IC50 (μM) (95% CI) | IC50 (μM) (95% CI) | IC50 (μM) (95% CI) | Ratio (95% CI) | ||
| MDMA | 0.447 (0.33–0.60) | 17 (12–24) | 1.36 (1.0–2.0) | 0.08 (0.04–0.16) | 100 |
| MBDB | 2.80 (1.9–4.1) | 22 (20–26) | 2.04 (1.4–3.0) | 0.09 (0.05–0.15) | 200 |
| MDEA | 1.02 (0.78–1.3) | 9.3 (8.0–11) | 1.27 (0.93–1.7) | 0.14 (0.01–0.21) | 125 |
| Ethylone | 2.54 (2.0–3.2) | 5.68 (4.9–6.5) | 4.46 (3.8–5.2) | 0.8 (0.6–1.1) | 175 |
| Mephedrone | 0.254 (0.22–0.30) | 3.31 (2.6–4.2) | 4.64 (3.7–5.9) | 1.4 (0.9–2.4) | 150 |
| Naphyrone | 0.25 (0.20–0.32) | 0.47 (0.40–0.55) | 0.96 (0.85–1.09) | 2.0 (1.5–2.7) | 25 |
| Butylone | 2.02 (1.5–2.7) | 2.90 (2.5–3.4) | 6.22 (4.3–9.0) | 2.1 (1.3–3.6) | 150 |
| Cocaine | 0.451 (0.38–0.59) | 0.768 (0.6–1.0) | 2.37 (2.0–2.9) | 3.1 (2–4.8) | 75 |
| Methylone | 0.542 (0.39–0.75) | 4.82 (3.8–6.1) | 15.5 (10–26) | 3.3 (1.5–6.8) | 150 |
| Flephedrone | 0.246 (0.16–0.37) | 6.35 (4.2–9.5) | >10 | 5.8 (0.8–41) | 200 |
| Cathinone | 0.199 (0.15–0.26) | 14.0 (10–20) | >100 | >10 | 50 |
| Methcathinone | 0.085 (0.06–0.17) | 1.12 (0.83–1.5) | >10 | >10 | 59 |
| Amphetamine | 0.094 (0.06–0.14) | 1.30 (0.83–2.0) | >10 | >10 | 30 |
| Methamphetamine | 0.064 (0.04–0.09) | 1.05 (0.74–1.5) | >10 | >10 | 30 |
| Pyrovalerone | 0.043 (0.03–0.06) | 0.035 (0.03–0.04) | 13.0 (10.8–15.8) | >100 | 20 |
| MDPV | 0.044 (0.03–0.07) | 0.031 (0.03–0.04) | 9.30 (6.8–12.8) | >100 | 5 |
Values are means of three to four independent experiments and 95% confidence intervals (CI).
Drugs are ranked according to the DAT/SERT ratio = 1/DAT IC50 : 1/SERT IC50.
*
Estimated average.