TFB-TBOA

Biological Activity

TFB-TBOA is a potent and selective glial glutamate transporter EAAT1 and EAAT2 inhibitor (IC₅₀ values are 17, 22 and 300 nM for EAAT2, EAAT1 and EAAT3, respectively). Exhibits selectivity for EAAT1 and EAAT2 over EAAT4 and EAAT5, and a wide range of neuronal receptors and transporters. In HEK293 cells expressing human EAAT1, 2, and 3, TFB-TBOA exhibited selectivity for hEAAT1 and hEAAT2 over hEAAT3 (respective IC₅₀ values are 3.6, 10, and 120 nM), while in tsA201 cells expressing rat EAAT4, [³H]-d-Asp uptake was inhibited with an IC₅₀ of 40 nM. Attenuates glutamate-stimulated intracellular Na⁺ elevation in astrocytes in vitro (IC₅₀ = 43 nM). Induces severe convulsions in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Glial glutamate transporter and glutamine synthetase regulate GABAergic synaptic strength in the spinal dorsal horn.
   Jiang E, Yan X, Weng HR
   J. Neurochem., 2012;121(4):526-36.
2. Functional Indicators of Glutamate Transport in Single Striatal Astrocytes and the Influence of Kir4.1 in Normal and Huntington Mice
   
   J Neurosci, 2016;36(18):4959-75.
3. Retinoic acid mediates the expression of glutamate transporter-1 in rat astrocytes through genomic RXR action and non-genomic protein kinase C signaling pathway.
   Chan TJ, Her LS, Liaw HJ, Chen MC, Tzeng SF
   J. Neurochem., 2012;121(4):537-50.
4. Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate.
   Bozzo and Chatton
   Brain Res., 2010;1316
5. Physical and functional interaction of NCX1 and EAAC1 transporters leading to glutamate-enhanced ATP production in brain mitochondria.
   Magi et al.
   PLoS One, 2012;7:e34015
6. Effects of a novel glutamate transporter blocker, (2S, 3S)-3-{3-[4-(trifluoromethyl)benzoylamino]benzyloxy}aspartate (TFB-TBOA), on activities of hippocampal neurons.
   Tsukada et al.
   Neuropharmacology, 2005;48:479
7. Elucidation of glutamate transporter functions using selective inhibitors.
   Shimamoto and Shigeri
   CNS Agents Med.Chem., 2006;6:59
8. Type I Interferon Receptor Signaling in Astrocytes Regulates Hippocampal Synaptic Plasticity and Cognitive Function of the Healthy CNS
   S Hosseini, K Michaelsen, G Grigoryan, C Chhatbar, U Kalinke, M Korte
   Cell Rep, 2020;31(7):107666.

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