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GMQ hydrochloride

2-GMQ hydrochloride, 2-Guanidine-4-methylquinazoline hydrochloride

An ASIC Channel Modulator and an ASIC3 Channel Opener

Cat #: G-165
Alternative Name 2-GMQ hydrochloride, 2-Guanidine-4-methylquinazoline hydrochloride
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 237.1
    Purity: >99%
    Effective concentration 1-5 mM.
    Chemical name 2-(4-methylquinazolin-2-yl)guanidine hydrochloride.
    Molecular formula C10H12ClN5.
    CAS No.: 5361-15-9
    PubChem CID 12253739
    Activity GMQ is an ASIC modulator, an ASIC3 opener and also induces an acidic shift of the pH dependence of inactivation of ASIC1a, -1b, -2a, and -31.
    1. Alijevic, O. and Kellenberger, S. (2012) J. Biol. Chem. 287, 36059.
    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 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs GMQ hydrochloride modulates ASIC3 channels expressed in Xenopus oocytes. 
      Alomone Labs GMQ hydrochloride modulates ASIC3 channels expressed in Xenopus oocytes. 
      Time course of ASIC3 currents elicited by stimulation with pH 6 every 50 sec, while membrane potential was held at -60 mV. 0.5 mM GMQ hydrochloride (#G-165), applied for 3.5 min, as indicated causes reversible complex effect combining peak amplitude depression with diminished inactivation, as seen with superimposed traces in B.
    References - Scientific background
    1. Alijevic, O. and Kellenberger, S. (2012) J. Biol. Chem. 287, 36059.
    2. Li, W.G. et al. (2010) Mol. Pain 88, 1186.
    3. Li, W.G. et al. (2011) J. Biol. Chem. 286, 42635.
    Scientific background

    2-guanidine-4-methylquinazoline (GMQ) is a small synthetic nonproton molecule that activates ASIC channels (acid-sensing ion channels). ASICs are proton-gated ion channels which are activated by a decrease in extracellular pH. GMQ is an activator of ASIC3 channels under physiological pH conditions; it induces a window current at pH 7.4 only in ASIC3. Evidence shows that GMQ alters the pH dependence of all ASIC subtypes studied1,2.

    GMQ contains basic groups that seem to form tight contacts with the carboxyl groups of acidic residues through hydrogen bonds (H-bonds) and electrostatic interactions that lead to the activation of ASIC3. In addition, GMQ contains a guanidinium group and a heterocyclic ring.

    Additional studies showed that GMQ activates sensory neurons and causes pain-related behaviors in an ASIC3-dependent manner3.

    Target ASIC1a, ASIC2, ASIC3
    Last update: 06/11/2022

    GMQ hydrochloride (#G-165) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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