R214127

A Potent, Selective, and Non-Competitive Antagonist of mGluR1
    Cat #: R-215
    Sizes: 5 mg, 10 mg, 25 mg, 50 mg
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 303.36 Da.
    Purity >98%.
    Effective concentration 10 nM – 10 µM.
    Structure
    Chemical name 1-(3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-2-phenylethanone.
    Molecular formula C20H17NO2.
    CAS number 409345-76-2.
    Activity R214127 is a potent and selective non-competitive antagonist of mGluR1 receptors, shown to inhibit rat mGluR1 mediated glutamate-induced Ca2+ mobilization with IC50 of 21.6 nM, whilst having no effect on rat mGluR5 at 10 µM1.
    Storage before reconstitution Product as supplied can be stored at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Reconstitution Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage after reconstitution -20°C.
    Our bioassay
    Alomone Labs R214127 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
    Dose response of R214127 (#R-215) normalized inhibition of human mGluR1-mediated, L-Glutamate-evoked Ca2+ mobilization.
    Cells were loaded with calcium-sensitive dye, incubated with a range of R214127 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™.
    References
    1. Lavreysen, H. et al. (2003) Mol. Pharmacol. 63, 1082.
    2. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
    Target: mGluR1
    Last update: 04/02/2018

    R214127 is a potent and selective non-competitive antagonist of mGluR1 displaying an IC50 value of 21.6 ± 5.0 nM1. The compound has minimal and nonspecific binding towards other mGlu receptors1.

    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), members of G-protein coupled receptors (GPCRs). These receptors are divided into three groups based on sequence homology 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 physiological functions including regulating ion channels, synaptic transmission and in synaptic plasticity that underlies learning and memory1,2.

    Alomone Labs is pleased to offer R214127 (#R-215).

    For research purposes only, not for human use