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DL-threo-β-Hydroxyaspartic acid is an inhibitor of excitatory amino acid transporters (EAATs).1,2 It inhibits glutamate uptake in COS-1 cells expressing human EAAT1 or EAAT2 (IC50s = 96 and 31 µM, respectively) as well as inward currents induced by L-aspartate in EAAT4-expressing Xenopus oocytes (Ki = 0.6 µM) and by L-glutamate in EAAT5-expressing oocytes (Ki = 2.5 µM) voltage-clamped at -60 mV. Intrathecal administration of DL-threo-β-hydroxyaspartic acid (7.5 and 15 µg/animal) reduces the number of flinches and shakes in the second phase of the formalin test in rats.3
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2. Effects of threo-
3. Effect of inhibition of spinal cord glutamate transporters on inflammatory pain induced by formalin and complete Freund’s adjuvant. Anesthesiology 114(2), 412-423 (2011).