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FPTQ

A Potent and Selective Antagonist of mGluR1 Receptors

Cat #: F-185
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 305.3
    Purity: >97%
    Effective concentration 10 nM – 10 µM.
    Structure
    Chemical name 6-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]quinolone.
    Molecular formula C17H12FN5.
    CAS No.: 864863-72-9
    PubChem CID 11301185
    Activity FPTQ is a selective allosteric antagonist of the mGluR1 receptors, inhibiting [3H]FTIDC binding with Ki of 14 nM, and inhibiting L-glutamate evoked Ca2+ mobilization with IC50 of 3.6 nM in CHO cells expressing human mGluR11. It specifically binds mGluR1 in the rat brain2.
    References-Activity
    1. Suzuki, G. et al. (2009) J. Pharmacol. Sci. 110, 315.
    2. Fujinaga, M. et al. (2011) Bioorg. Med. Chem. 19, 102.
    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 Up to 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs FPTQ inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs FPTQ inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Dose response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by FPTQ (#F-185), showing complete inhibition at 10 µM. hmGluR1-expressing cells were loaded with Ca2+-sensitive dye, incubated with a range of concentrations of FPTQ, and stimulated by 15 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Suzuki, G. et al. (2009) J. Pharmacol. Sci. 110, 315.
    2. Fujinaga, M. et al. (2011) Bioorg. Med. Chem. 19, 102.
    3. Satow, A. et al. (2008) J. Pharmacol. Exp. Ther.  326, 577.
    4. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    FPTQ is a synthetic compound that acts as a potent and selective allosteric antagonist of mGluR1 receptors. The compound shows very little inhibition of mGluR5 receptors. FPTQ shows high specific binding with mGluR1 receptor in the rat brain and displays IC50 values of 3.6 nM for human mGluR1 expressed in CHO cells1,2.

    Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) and play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly found in somatodendritic domains and postsynaptically regulate neuronal excitability and synaptic transmission through several intracellular second messenger systems3,4.

    Target mGluR1
    Last update: 12/08/2021

    FPTQ (#F-185) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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