Table 2.
Pharmacological characterization of analogs 3.1–3.12 as inhibitors at HEK293 cells stably expressing human EAAT1-3 in the [ 1 H]-D-aspartate uptake assay (Jensen & Bräuner-Osborne 2004 )
| ||||
|---|---|---|---|---|
| R 2 | EAAT1 | EAAT2 | EAAT3 | |
| (±)- endo-exo -3.1 |
|
>300 | >300 | >300 |
| (±)- endo-exo -3.2 |
|
>300 | >300 | >300 |
| (±)- endo-exo -3.3 |
|
>100 | >100 | >100 |
| (±)- endo-exo -3.4 |
|
>100 | ~100 | >300 |
| (±)- endo-exo -3.5 |
|
~300 | >300 | >300 |
| (±)- endo-exo -3.6 |
|
>100 | ~100 | >100 |
| (±)- endo-exo -3.7 |
|
~300 | ~300 | >300 |
| (±)- endo-exo -3.8 |
|
>300 | >300 | >300 |
| (±)- endo-exo -3.9 |
|
>300 | >300 | >300 |
| (±)- endo-exo -3.10 |
|
>300 | >300 | >300 |
| (±)- endo-exo -3.11 |
|
>300 | >300 | >300 |
| (±)- endo-exo -3n12 |
|
>100 | ~100 | >100 |
All values are given as IC50 in μM with pIC50 ± S.E.M. values in brackets (for the active analogs).












