Table 4. TSPO Ligands Based on 10a: Dependence of Rat Binding Affinity, Lipophilicity, and Genotype Sensitivity on Tether for Pendant Alkyl Carboxamido Group.
| ligand | X | rat Ki (nM)a | cLogD | LipE | LAB Ki (nM)b | HAB Ki (nM)c | (LAB Ki)/(HAB Ki) |
|---|---|---|---|---|---|---|---|
| 10m | CH2 | 0.9 ± 0.2 | 5.57 | 3.5 ± 0.1 | 53 ± 22 | 1.9 ± 0.5 | 27 ± 14 |
| 12 | S | 0.39 ± 0.04 | 5.31 | 4.10 ± 0.05 | 26 ± 5 | 2.5 ± 0.6 | 10 ± 3 |
| 14 | NH | 0.19 ± 0.01 | 4.11 | 5.62 ± 0.03 | 4 ± 1 | 0.44 ± 0.08 | 9 ± 3 |
| 15a | O | 0.070 ± 0.004 | 4.73 | 5.42 ± 0.03 | 1.3 ± 0.2 | 0.5 ± 0.2 | 2.5 ± 0.9 |
a
Mean SD for n = 6, except for 14 (n = 5).
b
Mean ± SD for n = 6, except for 10m (n = 5).
c
Mean ± SD for n = 6, except for 10m (n = 5).