DL-TBOA

DL-TBOA is an inhibitor of excitatory amino acid transporters (EAATs), with IC50 values of 67 and 5.5 µM for glutamate uptake in COS-1 cells expressing human EAAT1 and EAAT2, respectively. It 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. In vivo, DL-TBOA (500 µM, intrahippocampal perfusion) increases extracellular aspartate, glutamate, and alanine levels in rat hippocampus. Intrahippocampal injection of DL-TBOA increases lesion volume in the rat CA1 region in a dose-dependent manner and induces hyperexcitability, wet-dog shakes, salivation, forelimb myoclonus, limbic seizures, and epileptic EEG discharges at a dose of 25 nmol. DL-TBOA (5 and 10 µg, intrathecal) induces antinociception in the second phase of the formalin test in rats when administered 10 minutes prior to formalin.Formal Name: rel-3R-(phenylmethoxy)-D-aspartic acid. CAS Number: 205309-81-5. Synonyms: DL-threo-beta-Benzyloxyaspartate. Molecular Formula: C11H13NO5. Formula Weight: 239.2. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 100 mM, Water: 5mM with warming. SMILES: OC([C@@H](N)[C@@H](C(O)=O)OCC1=CC=CC=C1)=O. InChi Code: InChI=1S/C11H13NO5/c12-8(10(13)14)9(11(15)16)17-6-7-4-2-1-3-5-7/h1-5,8-9H,6,12H2,(H,13,14)(H,15,16)/t8-,9-/m0/s1. InChi Key: BYOBCYXURWDEDS-IUCAKERBSA-N.