TFB-TBOA

TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> EAAT2

Research Areas >> Neurological Disease

TFB-TBOA (CF3-Bza-TBOA) inhibits synaptically activated transporter currents (STCs) in astrocytes in the stratum radiatum in rat hippocampal slices in a dose-dependent manner with an IC50 of 13 nM, and reduces them to approximately 10% of the control at 100 nM[2]. TFB-TBOA inhibits the Na+i response evoked by 200 µM glutamate in a concentration-dependent manner with IC50 value of 43 nM, as measured on the amplitude of the Na+i response[1].

[1]. Shimamoto K, et al. Characterization of novel L-threo-beta-benzyloxyaspartate derivatives, potent blockers of the glutamate transporters. Mol Pharmacol. 2004;65(4):1008-1015.

[2]. Tsukada S, et al. Effects of a novel glutamate transporter blocker, (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA), on activities of hippocampal neurons. Neuropharmacology. 2005;48(4):479-491.

[3]. Bozzo L, et al. Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 2010;1316:27-34.