Table 1. Binding affinities (Ki) of TSPO ligands 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 | ||
| PK11195 | 36.0 ± 9.6 | 29.2 ± 10.3 | 1.2 |
| 1 (DPA-713) | 98.8 ± 2.3 | 19.5 ± 3.5 | 5.1 |
| 2 | 652.0 ± 223.0 | 114.0 ± 27.5 | 5.7 |
| 3 | 874.2 ± 206.2 | 207.6 ± 26.0 | 4.2 |