CGP-37849

A Potent and Selective Antagonist of NMDA Receptors
    Cat #: C-325
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source Synthetic
    MW: 209.14
    Purity: 98%
    Effective concentration 10-100 nM.
    Structure
    Chemical name (E)-2-amino-4-methyl-5-phosphonopent-3-enoic acid.
    Molecular formula C6H12NO5P.
    CAS No.: 127910-31-0.
    Activity CGP-37849 is a potent and selective antagonist of NMDA receptors, inhibiting the binding of selective NMDA ligand [3H]-CPP to rat brain NMDA with Ki of 35 nM. Orally bioavailable anticonvulsant in vivo1.
    Storage before reconstitution The product should be stored desiccated at +4°C.
    Reconstitution Soluble up to 50 mM in water. May require gentle warming. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage after reconstitution Store at -20°C. It is recommended to prepare solutions afresh on the day of use, or aliquot stock solutions stored at -20°C to prevent repeated thawing.
    Our bioassay
    Alomone Labs CGP-37849 inhibits NMDA receptor channels expressed in Xenopus oocytes.
    A. Representative time course of NR1/NR2A currents, elicited by transient stimulations with 50 µM glutamate + 50 µM glycine every 50 sec, while membrane potential was held at -60 mV. 4 min applications of 5 nM and 25 nM CGP-37849 (#C-325) reversibly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control, 5 nM and 25 nM CGP-37849 (as indicated).
    References
    1. Fagg, G.E. et al. (1990) Br. J. Pharmacol. 99, 791.
    2. Black, S.A. et al. (2014) Front. Cell Dev. Biol. 2, 45.
    Scientific background

    CGP-37849 is a synthetic compound that acts as a potent, selective, and competitive antagonist of N-methyl-d-aspartate (NMDA) receptors. CGP 37849 shows significant central effects following oral administration to animals. CGP-37849 is used to elucidate the roles of NMDA receptors in brain function, and as therapeutic agents for the treatment of neurological disorders such as epilepsy and ischemic brain damage in humans1.

    NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. They play important roles in a variety of cellular processes and brain functions such as synaptic plasticity, addiction, and stroke. NMDA receptor mediates physiological functions such as learning and memory formation and participates in glutamate excitotoxicity2.

    Target NMDA receptors
    Last update: 16/07/2018

    CGP-37849 (#C-325) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use