Cat. No. 2218
Chemical Name: (±)-3-Hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-6-carboxylic acid
Biological ActivityPotent, non-competitive excitatory amino acid transporter (EAAT) blocker. Preferentially inhibits glutamate-induced [3H]D-aspartate release (IC50 = 1.2 μM) rather than [3H]L-glutamate uptake (IC50 = 16.9 μM). Moderately selective; displays no affinity for NMDA and metabotropic glutamate receptors, and low affinity for AMPA and kainate receptors (IC50 values are 35 and 45 μM respectively).
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Conti et al (1999) Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists. J.Med.Chem. 42 4099. PMID: 10514280.
Conti et al (1999) Synthesis of new bicyclic analogues of glutamic acid. Tetrahedron 55 5623.
Funicello et al (2004) Dissociation of [3H]glutamate uptake from glutamate-induced [3H]D-Aspartate release by 3-hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-4-carboxylic acid and 3-hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-6-carboxylic acid, two conformationally constrained aspartate and glutamate analogs. Mol.Pharmacol. 66 522. PMID: 15322243.
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Keywords: HIP-B, supplier, Potent, non-competitive, EAAT, inhibitors, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter
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