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GYKI 53655 hydrochloride

An Antagonist of AMPA and Kainate Receptors

Cat #: G-220
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 388.85
    Purity: >99% (HPLC)
    Effective concentration 0.1-100 µM.
    Structure
    Chemical name 5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide;hydrochloride.
    Molecular formula C19H21ClN4O3.
    CAS No.: 143692-48-2
    PubChem CID 126757
    Activity GYKI 53655 hydrochloride, an analogue of GYKI 52466 hydrochloride (#G-125), is a non-competitive antagonist and negative allosteric modulator of AMPA receptors (GluR1 IC50 = 5.9 µM)1, selective over Kainate receptors (GluK3 IC50 = 63 µM)2. Exhibits anticonvulsant and neuroprotective activity both in vitro and in vivo3.
    References-Activity
    1. Bleakman, D. et al. (1996) Neuropharmacology 35,1689.
    2. Perrais, D. et al. (2009) Neuropharmacology 56, 131.
    3. Szabados, T. et al. (2001) Brain. Res. Bull. 55, 387.
    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 desiccated at +4°C.
    Solubility Soluble up to 100 mM in DMSO or water. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    It is recommended to aliquot stock solutions to prevent repeated thawing.
    Our bioassay
    • Alomone Labs GYKI 53655 hydrochloride inhibits GluA1 channels expressed in Xenopus oocytes. 
      Alomone Labs GYKI 53655 hydrochloride inhibits GluA1 channels expressed in Xenopus oocytes. 
      Representative time course of GluA1 current, activated by a continuous application (top dotted line) of 1 µM (S)-AMPA (#A-267), and reversibly inhibited by 50 µM GYKI 53655 hydrochloride (#G-220), as indicated (bar), at a holding potential of -80 mV.
    References - Scientific background
    1. Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843.
    2. Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843.
    3. Orav, E. et al. (2017) eNeuro 4, 3.
    Scientific background

    GYKI 53655 hydrochloride, a racemic 2,3-benzodiazepine is a AMPA and Kainate receptor antagonist. It acts as a non-competitive antagonist and negative allosteric modulator of AMPA receptors and is selective over Kainate receptors. It inhibits AMPA mediated responses in recombinant human GluA1 receptors expressed in HEK293 cells with an approximate IC50 values of 6 µM, and in recombinant human GluA4 expressing cells with an approximate IC50 values of 5 µM1. GYKI 53655 have been reported to be therapeutically effective in several animal models of epilepsy and global brain ischaemia1.

    The ionotropic glutamate AMPA receptors (AMPARs) are the primary receptors that mediate fast excitatory synaptic transmission in the mammalian brain. This function is essential for synaptic plasticity, learning, and memory1,2.

    Kainate receptors are highly expressed in the developing brain, where they are tonically activated to modulate synaptic transmission, network excitability, and synaptogenesis3.

    Target AMPA, Kainate receptors
    Lyophilized Powder
    Last update: 06/11/2022

    GYKI 53655 hydrochloride (#G-220) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
    Shipping and Ordering information

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