Table 1.
Monoamine transporter and receptor binding affinities
| NET | DAT | SERT | 5-HT1A | 5-HT2A | 5-HT2C | α1A | α2A | D1 | D2 | D3 | H1 | TA1rat | TA1mouse | |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| MDMA | 30.5 ± 8.0 | 6.5 ± 2.5 | 13.3 ± 0.6 | 12.2 ± 0.8 | 7.8 ± 2.4 | >13 | >6 | 15.0 ± 10 | >13.6 | 25.2 ± 12 | >17.7 | >14.4 | 0.37 ± 0.12 | 2.4 ± 1.1 |
| MBDB | 11.9 ± 1.4 | 3.1 ± 0.3 | 5.80 ± 0.7 | 15.5 ± 3.8 | 6.62 ± 1.8 | >13 | >6 | 16.9 ± 4 | >12.5 | NA | >16 | >13 | 1.2 ± 0.1 | 3.6 ± 1.1 |
| MDEA | 6.17 ± 1.4 | 1.35 ± 0.06 | 4.32 ± 0.6 | 18.8 ± 0.78 | >13 | >13 | >6 | 12.2 ± 0.5 | >12.5 | NA | >16 | >13 | 0.32 ± 0.6 | 4.9 ± 1.7 |
| Ethylone | 9.89 ± 0.9 | 1.43 ± 0.4 | 9.04 ± 0.6 | 17.0 ± 2.4 | >13 | >13 | >6 | >25 | >12.5 | NA | >16 | >13 | >12.5 | >10 |
| Mephedrone | >25 | 3.4 ± 0.8 | >30 | >20 | 2.1 ± 0.7 | >13 | 3.48 ± 2.2 | 11.0 ± 5.0 | >13.6 | >30 | >9.2 | >14.4 | 4.3 ± 2.0 | >10 |
| Naphyrone | 0.18 ± 0.02 | 0.04 ± 0.01 | 0.18 ± 0.02 | 6.00 ± 0.21 | 11 ± 2.2 | >13 | >6 | 8.0 ± 2.8 | >12.5 | NA | >16 | 2.28 ± 0.27 | >12.5 | >10 |
| Butylone | 8.13 ± 0.7 | 0.44 ± 0.03 | 14.1 ± 4.1 | >20 | >13 | >13 | >6 | >25 | >12.5 | NA | >16 | >13 | >12.5 | >10 |
| Cocaine | 4.47 ± 2.6 | 0.28 ± 0.07 | 1.1 ± 0.09 | >20 | >13 | >13 | >6 | >20 | >13.6 | >30 | >17.7 | >14.4 | >10 | >10 |
| Methylone | >25 | 2.73 ± 0.2 | >30 | >20 | >13 | >13 | >6 | >20 | >13.6 | >30 | >9.2 | >14.4 | >12.5 | >10 |
| Flephedrone | >25 | 12.2 ± 3.1 | >30 | >20 | 1.4 ± 0.6 | >13 | 1.52 ± 0.05 | >20 | >13.6 | >30 | >17.7 | >14.4 | 5.4 ± 1.7 | >10 |
| Cathinone | 3.50 ± 2.7 | 19.8 ± 1.9 | >30 | >20 | >13 | >13 | 5.40 ± 1.1 | 8.9 ± 2.7 | >13.6 | >30 | >17.7 | >14.4 | 2.2 ± 0.70 | 2.1 ± 0.73 |
| Methcathinone | 1.45 ± 0.7 | 1.28 ± 0.2 | >30 | 12.7 ± 3.5 | 3.0 ± 0.6 | >13 | 3.93 ± 1.3 | 11.9 ± 3.9 | >13.6 | >30 | >9.2 | >14.4 | 4.1 ± 1.2 | >10 |
| Amphetamine | 1.00 ± 0.6 | 5.68 ± 3.8 | >25 | 6.74 ± 1.38 | >13 | >13 | >6 | 2.8 ± 0.8 | >13.6 | >30 | >17.7 | >14.4 | 0.23 ± 0.18 | 0.09 ± 0.06 |
| Methamphetamine | 4.28 ± 2.1 | 1.85 ± 0.9 | 26.7 ± 11 | 8.07 ± 0.75 | >13 | >13 | >6 | 6.1 ± 1.6 | >13.6 | >30 | >17.7 | >14.4 | 0.35 ± 0.12 | 0.55 ± 0.2 |
| Pyrovalerone | 0.06 ± 0.005 | 0.03 ± 0.005 | 4.97 ± 0.3 | 13.4 ± 2.1 | >13 | >13 | >6 | >20 | >13.6 | >30 | >9.2 | 10.7 ± 1.5 | >12.5 | >10 |
| MDPV | 0.08 ± 0.02 | 0.01 ± 0.002 | 2.86 ± 0.1 | 10.29 ± 4.7 | >13 | >13 | >6 | >20 | >13.6 | >30 | >9.2 | >14.4 | 7.2 ± 1.1 | >10 |
Values are Ki given as μM (mean ± SD).
NA, not assessed.