Table 1 Pharmacological characterization of piperazine analogs 1 and 2.1-2.40 as inhibitors at HEK293 cells stably expressing human EAAT1-3 in the [ 3 H]-D-aspartate uptake assay (Jensen & Bräuner-Osborne 2004 )
| ||||
|---|---|---|---|---|
R1 | EAAT1 | EAAT2 | EAAT3 | |
(±)- exo -1 |
| 10 [5.03 ± 0.12] | 40 [4.44 ± 0.14] | 30 [4.78 ± 0.10] |
(±)- endo -1 |
| 14 [4.88 ± 0.09] | 32 [4.52 ± 0.12] | 10 [5.04 ± 0.13] |
(±)- endo-exo -1 |
| 14 [4.87 ± 0.08] | 42 [4.42 ± 0.11] | 14 [4.94 ± 0.16] |
2.1 |
| >300 | >300 | >300 |
2.2 |
| >300 | >300 | >300 |
2.3 |
| ~100 | ~100 | ~100 |
2.4 |
| >300 | >300 | >300 |
2.5 |
| >300 | >300 | >300 |
2.6 |
| >1000 | >300 | >300 |
2.7 |
| >1000 | >100 | >100 |
2.8 |
| >300 | >300 | >300 |
2.9 |
| >300 | >300 | >300 |
2.10 |
| >300 | >300 | >300 |
2.11 |
| ~150 | >100 | >100 |
2.12 |
| >100 | >100 | >100 |
2.13 |
| >300 | >300 | >300 |
2.14 |
| >300 | >300 | >300 |
2.15 |
| >300 | >300 | >300 |
2.16 |
| >100 | >100 | >100 |
2.17 |
| >300 | >300 | >1000 |
2.18 |
| >300 | >300 | >300 |
2.19 |
| >300 | >300 | >300 |
2.20 |
| >300 | >300 | >300 |
2.21 |
| >300 | >300 | >300 |
2.22 |
| ~100 | >100 | >100 |
2.23 |
| >300 | >300 | >100 |
2.24 |
| >100 | >100 | >100 |
2.25 |
| >300 | >100 | >300 |
2.26 |
| >300 | >300 | >300 |
2.27 |
| >300 | >300 | >300 |
2.28 |
| >300 | >300 | >300 |
2.29 |
| >300 | >100 | >100 |
2.30 |
| >300 | >1000 | >300 |
2.31 |
| >100 | >100 | >100 |
2.32 |
| >1000 | >300 | >300 |
2.33 |
| >1000 | >300 | >1000 |
(±)- endo-exo -2.34 |
| >300 | >300 | >300 |
2.35 |
| >300 | >300 | >1000 |
2.36 |
| >300 | >100 | >300 |
2.37 |
| >300 | >100 | >100 |
2.38 |
| >300 | >300 | >300 |
2.39 |
| >100 | >100 | >100 |
2.40 |
| >500 | >1000 | >500 |
