Table 5.
Fold increase and EC50 values of EAAT2 protein levels of selected analoguesa
 | |||||||
|---|---|---|---|---|---|---|---|
| Compound | R | Fold increase for EAAT2
|
EC50 (μM) | ||||
| 1 μM, 24 h | 10 μM, 24 h | ||||||
| β-actinb | GAPDHc | β-actinb | GAPDHc | β-actinb | GAPDHc | ||
| 7–4 | 2-Me-Bn | 1.0 ± 0.8 | 1.0 ± 0.3 | 3.5 ± 0.3 | 3.1 ± 0.2 | 2.6 ± 0.8 | 1.8 ± 0.3 |
| 7–7 | 2-Cl-Bn | 1.1 ± 0.5 | 1.6 ± 0.4 | 4.0 ± 0.3 | 4.5 ± 0.6 | 3.3 ± 0.5 | 3.2 ± 0.5 |
| 7–13 | 2,6-di-Me-Bn | 2.0 ± 0.2 | 2.0 ± 0.4 | 6.5 ± 1.0 | 6.4 ± 0.9 | 2.6 ± 0.2 | 2.4 ± 0.4 |
| 7–14 | 1-(2-Cl-6-F-phenyl)ethyl | 1.5 ± 0.5 | 1.8 ± 0.4 | 5.5 ± 1.0 | 5.2 ± 1.2 | 3.9 ± 0.5 | 2.4 ± 0.4 |
| 7–17 | 2,4-di-Me-Bn | 2.0 ± 0.3 | 2.2 ± 0.6 | 6.4 ± 1.0 | 6.0 ± 0.9 | 2.7 ± 0.3 | 1.8 ± 0.6 |
| 7–22 | 2,6-di-Cl-Bn | 3.0 ± 0.1 | 3.5 ± 0.0 | 3.9 ± 0.4 | 3.5 ± 0.5 | 0.5 ± 0.1 | 0.5 ± 0.0 |
| 7–16 | 2,4-di-F-Bn | 1.0 ± 0.2 | 1.0 ± 0.5 | 3.8 ± 0.8 | 3.7 ± 0.6 | 2.6 ± 0.2 | 2.6 ± 0.5 |
| 7–30 | 2,4,6-tri-Me-Bn | 1.5 ± 0.4 | 1.6 ± 0.4 | 4.7 ± 0.5 | 4.8 ± 0.6 | 2.4 ± 0.4 | 2.1 ± 0.4 |
| 7–15 | 2-(2-Cl-6-F-phenylethyl) | 1.2 ± 0.3 | 1.2 ± 0.2 | 6.7 ± 1.5 | 5.3 ± 1.2 | 3.3 ± 0.3 | 3.3 ± 0.2 |
| 7–31 | 2-(2-Cl-phenylethyl) | 1.0 ± 0.7 | 1.0 ± 0.1 | 4.8 ± 0.6 | 4.5 ± 0.6 | 4.7 ± 0.8 | 5.1 ± 0.1 |
| 7–33 | 1-(1,2,3,4-tetrahydronaphthalenyl) | 2.4 ± 0.3 | 2.8 ± 0.4 | 5.3 ± 1.1 | 4.5 ± 0.6 | 1.9 ± 0.3 | 1.7 ± 0.4 |
| 7–18 | 3-Cl-Bn | 4.0 ± 0.4 | 4.2 ± 0.1 | 4.1 ± 0.5 | 3.8 ± 0.5 | 1.7 ± 0.4 | 0.5 ± 0.1 |
a
Data represent the mean values of four separate experiments;
b
Data standardized by -actin;
c
Data standardized by GAPDH