Table 1.
List of the half-maximal inhibitory concentrations (IC50) of 4-benzylpiperidine carboxamides for SERT, NET, and DAT
| No | n | R1 | 5-HT | NE | DA |
|---|---|---|---|---|---|
| 7a | 3 | 3,5-dichlorophenyl | 0.19-0.84 | 0.12-0.56 | >10 |
| 7b | 3 | 2-indolyl | 0.24-0.92 | 0.12-0.56 | >10 |
| 7c | 3 | benzo(b)furanyl | 0.45-0.54 | 0.54-0.71 | >10 |
| 7d | 3 | benzo(b)thiophenyl | 0.32-0.61 | 0.98-10 | >10 |
| 7e | 3 | 4-biphenyl | 0.04-0.07 | 0.01-2.12 | >10 |
| 7f | 3 | diphenylacetyl | >10 | 0.83-3.38 | 0.09-0.40 |
| 7g | 3 | bis(4-chlorophenyl)acetyl | >10 | 1.13-3.62 | 0.78-2.34 |
| 7h | 3 | 2-quinolyl | 0.03-50 | 1.02-5.66 | >10 |
| 7i | 3 | 1-naphthyl | 7.51* | 0.87-7.43 | 8.09* |
| 7j | 3 | 2-naphthyl | 0.06-0.18 | 0.15-0.76 | >10 |
| 7k | 3 | 6-bromo-2-naphthyl | 0.31-46 | 0.53-1.45 | >10 |
| 7l | 3 | 6-methoxy-2-naphthyl | 0.23-0.45 | 0.02-2.72 | >10 |
| 8a | 2 | 3,5-dichlorophenyl | 0.55-6.22 | 0.55-1.88 | 0.37-1.17 |
| 8b | 2 | 2-indolyl | 0.15-1.12 | 0.20-3.82 | 0.34-1.68 |
| 8c | 2 | benzo(b)furanyl | 0.19-2.79 | 1.52-2.20 | 0.96-2.59 |
| 8d | 2 | benzo(b)thiophenyl | 0.18-5.39 | 0.60-1.26 | 0.84-2.13 |
| 8e | 2 | 4-biphenyl | 0.986* | 0.17-1.28 | > 10 |
| 8f | 2 | diphenylacetyl | >10 | 0.29-16 | 0.32-3.5 |
| 8g | 2 | bis(4-chlorophenyl)acetyl | > 10 | >10 | 0.195-2.05 |
| 8h | 2 | 2-quinolyl | 0.42-1.45 | 0.53-1.45 | > 10 |
| 8i | 2 | 1-naphthyl | >10 | 0.18-105 | 5.37* |
| 8j | 2 | 2-naphthyl | 0.39-1.31 | 0.28-0.57 | 0.71-3.70 |
| 8k | 2 | 6-bromo-2-naphthyl | 0.48-0.83 | 0.02-0.19 | 0.41-1.73 |
| 8l | 2 | 6-methoxy-2-naphthyl | 0.49-3.19 | 0.20-0.47 | 1.08-8.40 |
| - | - | Venlafaxine | 0.07-0.52 | 2.16-3.01 | - |
| - | - | GBR12909 | - | - | 0.02-0.08 |
The IC50 are shown as 95% confidence intervals. Unit of the concentration is μM.
*95% confidence interval could not be determined because the range was too wide.