Table 2.
Monoamine transporter and receptor-binding affinities
| NET | DAT | SERT | α1A | α2A | D1 | D2 | D3 | H1 | TA1rat | TA1mouse | |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Benzofurans | |||||||||||
| 5-APB | 3.1 ± 0.2 | 2.6 ± 0.3 | 3.2 ± 0.4 | 3.5 ± 0.5 | 2.9 ± 0.1 | <14 | <10 | <17 | 8.4 ± 0.8 | 0.04 ± 0.01 | 0.11 ± 0.01 |
| 5-APDB | 28 ± 5 | <30 | 4.0 ± 0.3 | 11 ± 3 | 4.2 ± 0.5 | <14 | <10 | <17 | 21 ± 2 | 0.49 ± 0.05 | 0.77 ± 0.06 |
| 6-APB | 1.8 ± 0.4 | 0.60 ± 0.05 | 12 ± 1 | 7.3 ± 3.4 | 0.38 ± 0.02 | <14 | <10 | <17 | 15 ± 2 | 0.05 ± 0.02 | 0.06 ± 0.02 |
| 6-APDB | 18 ± 1 | <30 | 23 ± 1 | <15 | 0.65 ± 0.07 | <14 | <10 | <17 | <25 | 1.0 ± 0.04 | 0.21 ± 0.04 |
| 5-MAPDB | 26 ± 5 | <30 | 6.3 ± 0.6 | 4.9 ± 1.5 | 6.4 ± 1.8 | 23 ± 3 | <10 | <17 | 4.9 ± 0.1 | 0.67 ± 0.09 | 3.5 ± 0.1 |
| 4-APB | 3.9 ± 0.5 | 7.4 ± 0.6 | 7.7 ± 0.5 | 12 ± 3 | 0.87 ± 0.22 | <14 | <10 | <17 | 16 ± 1 | 0.11 ± 0.02 | 2.08 ± 0.14 |
| 7-APB | 5.3 ± 0.1 | 14 ± 2 | 14 ± 1 | 9.6 ± 2.4 | 0.14 ± 0.02 | <14 | 8.2 ± 3.2 | <17 | 25 ± 5 | 0.07 ± 0.01 | 0.13 ± 0.02 |
| 5-EAPB | 1.0 ± 0.3 | 0.34 ± 0.02 | 0.52 ± 0.03 | 3.3 ± 0.5 | 2.7 ± 0.7 | 16 ± 3 | <10 | <17 | 2.4 ± 0.4 | 0.81 ± 0.08 | <15 |
| Benzodifuran | |||||||||||
| 2C-B-FLY | 17 ± 4 | <26 | 10 ± 3 | 11 ± 1 | 0.78 ± 0.3 | 1.4 ± 0.2 | 1.9 ± 0.3 | 6.8 ± 1.2 | 3.4 ± 0.5 | 0.03 ± 0.01 | 0.71 ± 0.23 |
| Related amphetamines | |||||||||||
| MDMAa | 27 ± 9 | 8.4 ± 3.3 | 13 ± 2 | <5 | 15 ± 10 | <12 | <20 | <17 | <13 | 0.37 ± 0.12 | 2.4 ± 1.1 |
| MDA | 13 ± 3.7 | <26 | 5.6 ± 1.5 | <5 | 1.1 ± 0.1 | <12 | <20 | <17 | <13 | 0.25 ± 0.04 | 0.16 ± 0.01 |
| β-Keto-MDA | <30 | 11 ± 2 | <30 | <5 | 15 ± 2 | <12 | <20 | <17 | <13 | 4.8 ± 0.9 | 6.5 ± 2.8 |
| Methamphetaminea | 3.0 ± 2.2 | 1.8 ± 0.7 | 25 ± 10 | <5 | 6.1 ± 1.6 | <12 | <20 | <17 | <13 | 0.35 ± 0.12 | 0.55 ± 0.24 |
Values are Ki given as μM (mean ± SD).
a
Values are from Simmler et al., 2014a.