EAAT1 和 EAAT2 抑制剂
TFB-TBOA is an inhibitor of excitatory amino acid transporter 1 (EAAT1) and EAAT2 with IC50 values of 22 and 17 nM for EAAT1 and EAAT2, respectively, in a glutamate uptake assay using COS-1 cells.1 It is selective for EAAT1 and EAAT2 over EAAT3 (IC50 = 300 nM), as well as the choline, dopamine, GABA, norepinephrine, and serotonin transporters and a variety of neurotransmitter receptors at 10 µM. TFB-TBOA (10 µM) inhibits L-glutamate- and L-aspartate-induced currents in X. laevis oocytes. It induces convulsions in mice when administered at a dose of 0.2 µg/animal.
1.Shimamoto, K., Sakai, R., Takaoka, K., et al.Characterization of novel L-threo-β-benzyloxyaspartate derivatives, potent blockers of the glutamate transportersMol. Pharmacol.65(4)1008-1015(2004)
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