Name: DL-TBOA
Price: 514.00 USD

- Overview
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    Background
    
    Ki: 42 μM for EAAT1; 5.7 μM for EAAT2Glutamate acts as an excitatory neurotransmitter in the mammalian central nervous system and a potent neurotoxin. Glutamate transporters also play an important role in maintaining the extracellular glutamate concentration below neurotoxic levels and therefore contribute to the prevention of neuronal damage. DL-TBOA was synthesized and examined as an inhibitor of sodium-dependent glutamate/aspartate transporters(excitatory amino acid transporters).In vitro: DL-TBOA inhibited the uptake of [14C]glutamate in COS-1 cells overexpressing the human excitatory amino acid transporter-1 (EAAT1) (Ki = 42 μM) with almost the same potency as DL-threo-b-hydroxyaspartate (Ki = 58 μM). With regard to the human excitatory amino acid transporter-2 (EAAT2), the inhibitory effect of DL-TBOA (Ki = 5.7 μM) was much more potent than that of dihydrokainate (Ki = 79 μM), which is well known as a selective blocker of this subtype. [1]. In vivo: Microdialysis administration of 500 μM DL-TBOA into the hippocampus increased 3.4- and nine-fold the extracellular levels of aspartate and glutamate, respectively. Upon stereotaxic administration it induced neuronal damage dose-dependently in CA1 and dentate gyrus, and convulsive behavior. Electroencephalographic recording showed limbic seizures appearance in the hippocampus after DL-TBOA infusion. [2]. Clinical trial: Up to now, DL-TBOA is still in the preclinical development stage.
    
    [1] Shimamoto K, Lebrun B, Yasuda-Kamatani Y, Sakaitani M, Shigeri Y, Yumoto N, Nakajima T. DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. Mol Pharmacol. 1998 Feb;53(2):195-201.
    [2] Montiel T, Camacho A, Estrada-Sánchez AM, Massieu L. Differential effects of the substrate inhibitor l-trans-pyrrolidine-2,4-dicarboxylate (PDC) and the non-substrate inhibitor DL-threo-beta-benzyloxyaspartate (DL-TBOA) of glutamate transporters on neuronal damage and extracellular amino acid levels in rat brain in vivo. Neuroscience. 2005;133(3):667-78.
- Properties
  - Alternative Name
    
    (2S,3S)-2-amino-3-(benzyloxy)succinic acid
    
    CAS Number
    
    205309-81-5
    
    Molecular Formula
    
    C11H13NO5
    
    Molecular Weight
    
    239.23
    
    Appearance
    
    White solid
    
    Purity
    
    98.00%
    
    Solubility
    
    <23.92mg/ml in DMSO;insoluble in H2O
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only

DL-TBOA

DL-TBOA

Background

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