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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 )

From: Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the Excitatory Amino Acid Transporters (EAATs): improving the potency of a micromolar screening Hit is not truism

  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
  1. All values are given as IC50 in μ M with pIC50 ± S.E.M. values in brackets (for the active analogs).