An EAAT inhibitor (IC50s = 67 and 5.5 μM for glutamate uptake in COS-1 cells expressing human EAAT1 and EAAT2

DL-TBOA – 10 mg

Brand:
Cayman
CAS:
205309-81-5
Storage:
-20
UN-No:
Non-Hazardous - /

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.{45698} 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.{45699} In vivo, DL-TBOA (500 μM, intrahippocampal perfusion) increases extracellular aspartate, glutamate, and alanine levels in rat hippocampus.{45700} 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.{45701}  

 

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SKU: 29632 - 10 mg Category:

Description

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

Formal name: rel-3R-(phenylmethoxy)-D-aspartic acid

Synonyms:  DL-threo-β-Benzyloxyaspartate

Molecular weight: 239.2

CAS: 205309-81-5

Purity: ≥98%

Formulation: A solid

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