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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).