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GYKI 52466 hydrochloride

An Antagonist of AMPA and Kainate Receptors

Cat #: G-125
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 329.78
    Purity: >96.6%
    Form Lyophilized powder.
    Effective concentration 300 nM - 300 µM.
    Structure
    Chemical name 1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride.
    Molecular formula C17H16ClN3O2.
    CAS No.: 192065-56-8
    Activity GYKI 52466 is a selective allosteric AMPA/kainate receptor antagonist, with an IC50 of ~10 μM for AMPA induced currents in cultured superior colliculus neurons1.
    References-Activity
    1. Rammes, G. et al. (1996) Br. J. Pharmacol.  117, 1209.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 30 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs GYKI 52466 hydrochloride blocks GluA1 receptors expressed in Xenopus oocytes.
      Alomone Labs GYKI 52466 hydrochloride blocks GluA1 receptors expressed in Xenopus oocytes.
      A. Time course of 300 μM GYKI 52466 hydrochloride (#G-125) reversible inhibitory action on glutamate-elicited currents (100 μM, delivered every 100 seconds, holding potential -60 mV). B. Superimposed current traces of control and inhibited current as indicated (taken from the experiment in A).
    References - Scientific background
    1. Szabados, T.  et al. (2001) Brain Res. Bull. 55, 387.
    Scientific background GYKI 52466 hydrochloride is a non-competitive AMPA and kainate receptor antagonist. It blocks GluK3 homomeric receptors with an IC50 of 63 μM and GluK2b(R)/GluK3 heteroreceptors with an IC50 of 32 μM at high concentrations. GYKI 52466 has been reported to prevent the excitotoxic action of high extracellular glutamate levels due to its potent non-competitive AMPA receptor antagonistic effect. It has been demonstrated histologically that GYKI 52466 has neuroprotective actions in experimental models of global and focal cerebral ischaemia. The compound was widely investigated in experimental seizure models, where it provided effective protection against convulsions evoked by chemical agents such as AMPA or kainate, electroshock and audiogenic stimulation1.
    Target AMPA/Kainate receptors
    Lyophilized Powder
    Last update: 02/01/2022

    GYKI 52466 hydrochloride (#G-125) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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