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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 )

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

  R2 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
  1. All values are given as IC50 in μ M with pIC50 ± S.E.M. values in brackets (for the active analogs).