(±)-threo-3-Methylglutamic acid is a potent blocker of glutamate transport. (±)-threo-3-Methylglutamic acid is selective for EAAT2 and EAAT4 (IC50 values are 90, 109, 1600 and 1080 μM for EAAT2, EAAT4, EAAT1 and EAAT3 respectively).
Vandenberg et al (1997) Contrasting modes of action of methylglutamate derivatives on the excitatory amino acid transporters, EAAT1 and EAAT2. Mol.Pharmacol. 51 809. Mitrovic et al (1998) Identification of functional domains of the human glutamate transporters EAAT1 and EAAT2. J.Biol.Chem. 273 14698. Eliasof et al (2001) Pharmacological characterization of threo-3-methylglutamic acid with excitatory amino acid transporters in native and recombinant systems. J.Neurochem. 77 550.
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