Table 4.3.
Binding affinities of piperazine-based modafinil analogs
| Compound | X | Y | Z | R | DAT (Ki, nM) |
NET (Ki, nM) | SERT (Ki, nM) |
|---|---|---|---|---|---|---|---|
| 5q | H | S=O | C=O | 3-phenylpropyl | 33.0 ± 2.83 | 54300 ± 3210 | 15200 ± 1100 |
| 5r | 4,4′-diF | S=O | C=O | 3-phenylpropane | 37.6 ± 1.86 | 12000 ± 1430 | 1320 ± 152 |
| 5s | 4,4′-diF | S=O | C=O | 2-OH-propyl | 752 ± 87.4 | NA | 32800 ± 4430 |
| 5t | 3,3′-diCl | S=O | C=O | 2-OH-propyl | 1380 ± 191 | >50 uM | NA |
| 5u | H | S | C | 2-OH-propyl | 49.6 ± 4.31 | 44500 ± 2400 | 26700 ± 2630 |
| 5v (JJC8-091) | 4,4′-diF | S | C | 2-OH-propyl | 16.7 ± 1.22 | 17800 ± 885 | 1770 ± 234 |
| 5w (JJC8-088) | 4,4′-diF | S | C | 2-OH, 3-phenylpropyl | 6.72 ± 0.977 | 1950 ± 227 | 213 ± 13.2 |