DL-TBOA

An EAAT inhibitor (IC50s = 67 and 5.5 µM for glutamate uptake in COS-1 cells expressing human EAAT1 and EAAT2, respectively); inhibits inward currents induced by L-aspartate in EAAT4-expressing Xenopus oocytes (Ki = 4.4 µM) and by L-glutamate in EAAT5-expressing oocytes (Ki = 3.2 µM) voltage-clamped at -60 mV; increases extracellular aspartate, glutamate, and alanine levels in rat hippocampus at 500 µM; increases lesion volume in the rat hippocampal CA1 region when administereed intrahippocampally; induces hyperexcitability, wet-dog shakes, salivation, forelimb myoclonus, limbic seizures, and epileptic EEG discharges in rats at 25 nmol; induces antinociception in the second phase of the formalin test in rats at 5 and 10 µg when administered 10 minutes prior to formalin