Table 1.
Monoamine transporter inhibition
| NET | DAT | SERT | DAT/SERT inhibition ratio | |
|---|---|---|---|---|
| IC50 (μM) (95% CI) | IC50 (μM) (95% CI) | IC50 (μM) (95% CI) | Ratio (95% CI) | |
| Benzofurans | ||||
| 5-APB | 0.16 (0.08–0.3) | 6.1 (4–9) | 0.29 (0.17–0.5) | 0.05 (0.02–1.2) |
| 5-APDB | 0.29 (0.2–0.5) | 49 (33–73) | 0.58 (0.4–0.9) | 0.01 (0.005–0.03) |
| 6-APB | 0.19 (0.1–0.3) | 3.3 (2.4–4.5) | 0.93 (0.7–1.3) | 0.29 (0.16–0.54) |
| 6-APDB | 0.56 (0.4–0.8) | 33 (25–43) | 2.3 (1.4–3.9) | 0.07 (0.03–0.16) |
| 5-MAPDB | 0.96 (0.5–1.7) | 77 (62–96) | 1.2 (0.7–2) | 0.02 (0.01–0.03) |
| 4-APB | 0.24 (0.2–0.3) | 12 (9–16) | 5.5 (3.4–8.7) | 0.46 (0.21–1.0) |
| 7-APB | 0.27 (0.2–0.3) | 20 (16–26) | 13 (9–18) | 0.65 (0.35–1.1) |
| 5-EAPB | 0.56 (0.4–0.7) | 4.9 (3–8) | 0.72 (0.5–1.1) | 0.15 (0.07–0.35) |
| Benzodifuran | ||||
| 2C-B-FLY | 94 (72–124) | 187 (161–217) | 73 (58–92) | 0.39 (0.27–0.57) |
| Related amphetamines | ||||
| MDMA | 0.36 (0.2–0.6) | 16.7 (16.3–17) | 2.4 (1.4–3.0) | 0.14 (0.08–0.18) |
| MDA | 0.42 (0.3–0.6) | 20.5 (20.3–20.6) | 4.9 (3.5–6.8) | 0.24 (0.17–0.33) |
| β-Keto-MDA | 1.6 (1.1–2.3) | 14 (10–18) | 21 (15–28) | 1.5 (0.8–2.8) |
| Methamphetamine | 0.14 (0.09–0.2) | 0.87 (0.84–0.91) | 13.6 (13.5–13.8) | 15.6 (14.8–16.4) |
Values are means of three to four independent experiments and 95% confidence intervals (CI). DAT/SERT inhibition ratio = 1/DAT IC50: 1/SERT IC50.