Table 3.
| ||||
---|---|---|---|---|
Compound | X | R | Fold increase for EAAT2a |
|
4 h | 24 h | |||
1 | S | 2-Cl-6-F-Bn | nab | 2.0 ± 0.8 |
8–2 | O | 2-Cl-6-F-Bn | 1.1 ± 0.3 | 2.9 ± 0.4 |
7–4 | S | 2-Me-Bn | 1.7 ± 0.1 | 3.5 ± 0.3 |
8–1 | O | 2-Me-Bn | 2.0 ± 0.9 | 2.5 ± 0.5 |
7–13 | S | 2,6-di-Me-Bn | na | 6.5 ± 1.0 |
8–3 | O | 2,6-di-Me-Bn | 2.1 ± 1.2 | 3.2 ± 1.4 |
7–14 | S | 1-(2-Cl-6-F-phenyl)ethyl | 1.7 ± 0.9 | 5.5 ± 1.0 |
8–4 | O | 1-(2-Cl-6-F-phenyl)ethyl | 1.6 ± 0.2 | 3.0 ± 0.7 |
7–15 | S | 2-(2-Cl-6-F-phenylethyl) | 1.9 ± 0.7 | 6.7 ± 1.5 |
8–5 | O | 2-(2-Cl-6-F-phenylethyl) | 2.2 ± 0.4 | 3.1 ± 1.2 |
7–16 | S | 2,4-di-F-Bn | 2.4 ± 1.5 | 3.8 ± 0.8 |
8–6 | O | 2,4-di-F-Bn | na | 2.3 ± 0.6 |
7–17 | S | 2,4-di-Me-Bn | 1.9 ± 0.8 | 6.4 ± 1.0 |
8–7 | O | 2,4-di-Me-Bn | na | 2.0 ± 0.9 |
6–1 | S | H | na | 2.0 ± 0.8 |
5–1 | O | H | 1.5 ± 0.5 | 1.6 ± 1.0 |
14 | NH | 2-Me-Bn | 1.7 ± 1.1 | 2.6 ± 0.5 |
9–1 | SO2 | 2-Cl-6-F-Bn | 1.4 ± 0.3 | 2.8 ± 0.4 |
9–2 | SO2 | 2-Me-Bn | 2.3 ± 0.4 | 1.1 ± 0.2 |
9–3 | SO2 | 2-Cl-Bn | 1.6 ± 0.3 | na |
17–1 | CONH | n-Pr | na | 1.2 ± 0.2 |
17–2 | CONH | 2-Me-Bn | na | 1.4 ± 0.2 |
Compound concentration of 10 μM;
na = not active