Table 3. Binding affinities (Ki) of acetanilides at wild type and A147T TSPO-expressing HEK-293 membranes. The affinity of all compounds was indexed by the displacement of [3H] PK-11195 (10 nM) in radioligand binding assays. Values represent the mean ± SD from at least three independent experiments performed in duplicate.
| Compound |
K
i (nM) |
A147T : wild type | |
| A147T | Wild type | ||
| 17 | 1262.0 ± 170.2 | 275.5 ± 121.8 | 4.6 |
| 18 | 2785.0 ± 361.1 | 500.3 ± 134.0 | 5.6 |
| 19 | 3933.0 ± 1092.0 | 275.0 ± 87.8 | 14.3 |
| 20 | 3147.0 ± 596.1 | 823.0 ± 247.7 | 3.8 |
| 21 | 737.8 ± 46.6 | 376.8 ± 82.2 | 2.0 |
| 22 | 4255 ± 741.4 | 1009.6 ± 287.3 | 4.2 |
| 23 | 4211 ± 1370.8 | 1198.3 ± 333.2 | 3.5 |
| 24 | >10 000 | 1293.3 ± 80.1 | >7.7 |
| 25 | >10 000 | 2243.3 ± 560.9 | >4.5 |
| 26 | 1770.7 ± 125.3 | 433.2 ± 95.8 | 4.2 |