Table 3.
5-HT receptor interactions
| 5-HT1A | 5-HT2A | 5-HT2B | 5-HT2C | ||||
|---|---|---|---|---|---|---|---|
| Receptor-binding Ki (μM) | Receptor-binding Ki (μM) | Activation potency EC50 (μM) | Activation efficacy % maximum | Activation potency EC50 (μM) | Activation efficacy % maximum | Receptor-binding Ki (μM) | |
| Benzofurans | |||||||
| 5-APB | 3.3 ± 0.2 | 0.84 ± 0.27 | 6.3 ± 2.1 | 54 ± 35 | 0.28 ± 0.12 | 61 ± 17 | 0.88 ± 0.33 |
| 5-APDB | 20 ± 4 | 3.4 ± 1.0 | 11 ± 2 | 24 ± 17 | 1.2 ± 0.6 | 50 ± 21 | 0.06 ± 0.02 |
| 6-APB | 1.5 ± 0.2 | 0.97 ± 0.23 | 5.9 ± 1.8 | 43 ± 23 | 0.14 ± 0.06 | 70 ± 9 | 0.27 ± 0.05 |
| 6-APDB | 9.2 ± 1.5 | 2.0 ± 1.0 | 5.9 ± 1.1 | 62 ± 36 | 0.12 ± 0.03 | 66 ± 17 | 0.06 ± 0.02 |
| 5-MAPDB | 26 ± 6 | 4.8 ± 2.1 | <20 | 0 | <20 | 0 | 0.10 ± 0.02 |
| 4-APB | 1.2 ± 0.1 | 0.96 ± 0.17 | 13 ± 2 | 30 ± 9 | 1.0 ± 0.5 | 38 ± 16 | 0.06 ± 0.02 |
| 7-APB | 0.28 ± 0.05 | 0.91 ± 0.20 | 5.7 ± 2.0 | 43 ± 21 | 0.28 ± 0.52 | 52 ± 17 | 3.3 ± 0.3 |
| 5-EAPB | 3.1 ± 0.6 | 2.7 ± 1.5 | 7.6 ± 3.2 | 29 ± 7 | <20 | 0 | 4.6 ± 1.3 |
| Benzodifuran | |||||||
| 2C-B-FLY | 0.35 ± 0.04 | 0.011 ± 0.002 | 0.0015 ± 0.0002 | 82 ± 12 | 0.040 ± 0.036 | 56 ± 3 | 0.012 ± 0.004 |
| Related amphetamines | |||||||
| MDMA | 12 ± 0.8a | 6.3 ± 2.4 | 6.1 ± 0.3 | 55 ± 9 | <20 | 0 | <13a |
| MDA | 4.9 ± 0.9 | 3.3 ± 0.8 | 0.63 ± 0.24 | 77 ± 16 | 0.85 ± 0.11 | 52 ± 12 | 3.0 ± 0.9 |
| β-Keto-MDA | <17 | <13 | <20 | 0 | <20 | 0 | <13 |
| Methamphetamine | 8.1 ± 0.7a | <13 | <20 | 0 | <20 | 0 | <13a |
Values are Ki given as μM (mean ± SD).
a
Values are from Simmler et al., 2014a and were included for comparison.