Cat. No. 2217
Chemical Name: (±)-3-Hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-4-carboxylic acid
Biological ActivityPotent, non-competitive excitatory amino acid transporter (EAAT) blocker. Preferentially inhibits glutamate-induced [3H]D-aspartate release (IC50 = 1.6 μM) rather than [3H]L-glutamate uptake (IC50 = 18 μM). Moderately selective; displays no affinity for NMDA and metabotropic glutamate receptors, and low affinity for AMPA and kainate receptors (IC50 values are 43 and 8 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-A, supplier, Potent, non-competitive, EAAT, inhibitors, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter
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