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NPS 2390

A Potent and Selective Antagonist of mGluR1 and mGluR5 Receptors
Cat #: N-340
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 307.4
    Purity: >98%
    Effective concentration 10 nM – 1 uM.
    Structure
    Chemical name N-(1-adamantyl)quinoxaline-2-carboxamide.
    Molecular formula C19H21N3O.
    CAS No.: 226878-01-9.
    PubChem CID 7067728
    Activity NPS 2390, a quinoxaline derivative, is a potent and selective non-competitive antagonist of Group I mGluRs, acting on mGluR1 and mGluR5 with IC50 values of to 5.2 and 82 nM, respectively, while having no effect on mGluR2, mGluR8 and other targets at 30 μM1-3.
    References-Activity
    1. Mabire, D. et al. (2005) J. Med. Chem48, 2134.
    2. Lavreysen, H. et al. (2003) Mol. Pharmacol63, 1082.
    3. Van Wagenen, B.C. et al. (2000) Abstr. Soc. Neurosci. Presentation No. 618, 3.
    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 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs NPS 2390 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs NPS 2390 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Dose response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by NPS 2390 (#N-340). IC50 was determined at 56.7 nM. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of concentrations of NPS 2390, 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. Mabire, D. et al. (2005) J. Med. Chem48, 2134.
    2. Lavreysen, H. et al. (2003) Mol. Pharmacol63, 1082.
    3. Van Wagenen, B.C. et al. (2000) Abstr. Soc. Neurosci. Presentation No. 618, 3.
    4. O'Brien, J.A. et al. (2003) Mol. Pharmacol. 64, 731.
    5. Satow, A. et al. (2008) J. Pharmacol. Exp. Ther. 326, 577.
    6. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    7. Lu, Y.M. et al. (1996) J. Neurosci. 17, 5196.
    Scientific background

    NPS 2390, a quinoxaline derivative, is a synthetic, potent, selective and non-competitive antagonist of group I metabotropic glutamate receptors comprising mGluR1 and mGluR5 receptors with IC50 values of 5.2 and 8.2 nM respectively7. The compound shows very low affinity towards other mGluR receptors.

    Several studies suggest that NPS 2390 acts on a site that is different from the glutamate binding pocket. It is likely that the compound acts at the transmembrane segment VII region of the receptors1-3.

    Metabotropic glutamate receptors (mGluRs) are G protein coupled receptors (GPCR) that 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 systems4,5. The mGlu1 receptors play an important role in motor learning and motor coordination whereas mGlu5 receptors contribute to induction of long-term potentiation and associative learning6.

    Target mGluR1, mGluR5 receptors
    Last update: 23/08/2020

    NPS 2390 (#N-340) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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