Chemical Name: 3-((4-Cyclohexylpiperazin-1-yl)(1-phenethyl-1H-tetrazol-5-yl)methyl)-6-methoxyquinolin-2(1H)-one
Biological ActivityPotent and selective EAAT2 positive allosteric modulator (EC50 = 0.26 nM). Enhances the glutamate translocation rate, with no effect on substrate interaction. Enhances glutamate uptake by cultured astrocytes by approximately 58%. Exhibits no significant effect on DAT, SERT and NET or NMDA receptors.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Identification of novel allosteric modulators of glutamate transporter EAAT2.
Kortagere et al.
ACS Chem Neurosci., 2018;9:522
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