A-841720

An Antagonist of mGluR1 and mGluR5
Cat #: A-440
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 343.45
    Purity: >98%
    Effective concentration 1-100 nM.
    Chemical name 3-(azepan-1-yl)-9-(dimethylamino)pyrido[1,2]thieno[3,4-d]pyrimidin-4-one.
    Molecular formula C17H21N5OS.
    CAS No.: 869802-58-4.
    Activity A-841720 is a potent and selective non-competitive mGluR1 antagonist, acting on mGluR1 and mGluR5 with IC50 values of 10 nM and 342 nM, respectively1in vivo it shows analgesic properties, significantly attenuating spontaneous post-operative pain behavior in rats (ED50 = 10 μmol/kg) 2.
      • Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.

      • Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314.

    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. Protect from light and moisture.
    Solubility Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
      • Alomone Labs A-841720 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
        Dose response of A-841720 (#A-440) normalized inhibition of human mGluR1-mediated, L-Glutamate evoked Ca2+ mobilization. Cells were loaded with calcium-sensitive dye, incubated with a range of A-841720 concentrations, and stimulated with 5 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was determined at 3.86 nM.
      • Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
      • Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314.
      • A-841720 is a non-competitive and potent antagonist of mGluR11,2 with an IC50 value of 10 nM1. At higher concentrations, it also inhibits mGluR5 receptors displaying an IC50 value of 342 nM1.

        Glutamate is the most abundant excitatory neurotransmitter in the central nervous system and it modulates activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs). mGluRs consist of three groups: I, II, and III with a total of eight subtypes, mGluR1 to mGluR8. mGluR1 plays an important role in the central sensitization of pain and in a variety of functions with potential implications in neurological and psychiatric disorders1,2.

    Target mGluR1, mGluR5
    Last update: 18/02/2019

    A-841720 (#A-440) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use