Discontinued Product

2217 has been discontinued.
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(±)-HIP-A | CAS No. 227619-64-9 | Glutamate (EAAT) Transporter Inhibitors
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Description: Potent, non-competitive EAAT inhibitor

Chemical Name: (±)-3-Hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-4-carboxylic acid

Purity: ≥98%

Product Details

Biological Activity

Potent, 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). .

Technical Data

Soluble to 10 mM in water
Store at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.
    Conti et al.
    J.Med.Chem., 1999;42:4099
  2. Synthesis of new bicyclic analogues of glutamic acid.
    Conti et al.
    Tetrahedron, 1999;55:5623
  3. 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-pyrro
    Funicello et al.
    Mol.Pharmacol., 2004;66:522

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