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PEAQX tetrasodium hydrate

NVP-AAM077

An Antagonist of NMDA Receptors

Cat #: P-255
Alternative Name NVP-AAM077
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 560.15
    Purity: >95%
    Form Lyophilized powder.
    Effective concentration 10 nM - 1 µM.
    Structure
    Chemical name tetrasodium;5-[[[(1S)-1-(4-bromophenyl)ethyl]amino]-phosphonatomethyl]quinoxaline-2,3-diolate;hydrate.
    Molecular formula C17H15BrN3Na4O6P.
    CAS No.: 459836-30-7
    PubChem CID 71311756
    Activity PEAQX is an NMDA receptor antagonist1.
    References-Activity
    1. Frizelle, P.A. et al. (2006) Mol. Pharmacol. 70, 1022.
    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 100 mM in water. Centrifuge all product preparations before use (10,000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs PEAQX tetrasodium hydrate inhibits NMDA (NR1+NR2A) receptors expressed in Xenopus oocytes. 
      Alomone Labs PEAQX tetrasodium hydrate inhibits NMDA (NR1+NR2A) receptors expressed in Xenopus oocytes. 
      A. Time course of NMDA currents elicited with 25 µM glutamate and 25 µM Glycine, every 50 sec, while membrane potential was held at -80 mV. 0.1 µM PEAQX tetrasodium hydrate (#P-255), applied for 2.5 min as indicated, inhibited current amplitude. B. Superimposed current traces taken from the experiment described in A.
    References - Scientific background
    1. Frizelle, P.A. et al. (2006) Mol. Pharmacol. 70, 1022.
    2. de Marchena, J. et al. (2008) J. Neurophysiol. 100, 1936.
    3. Black, S.A. et al. (2014) Front. Cell. Dev. Biol. 2, 45.
    Scientific background

    PEAQX tetrasodium hydrate (NVP-AAM007) is a competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. This compound shows higher selectivity for NR2A over NR2B subunit-containing receptor. PEAQX IC50 values are strongly dependent on agonist concentration used to evoke response. IC50 for NR1/NR2A were 31 ± 2 nM for EC50 of glutamate, and 214 ± 10 nM for 10-times the EC50 of glutamate. IC50 values for NR1/NR2B were significantly higher: 215 ± 13 nM and 2.2 ± 0.14 μM for EC50 and 10-times the EC50 of glutamate, respectively1.

    Several studies claim that PEAQX has the ability to cause a blockade of adult long-term potentiation while only moderately affecting juvenile long-term potentiation. It was shown that subsaturating concentrations of APV (a NMDAR antagonist) can imitate the effects of PEAQX on long-term potentiation. These findings suggest that the synaptic plasticity affected by PEAQX can be explained by nonspecific blockade of NMDA receptors2.

    NMDA receptors play an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. NMDA receptors mediate several physiological functions including learning and memory formation; they play a role in glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease3.

    Target NR1, NR2 receptors
    Last update: 08/06/2021

    PEAQX tetrasodium hydrate (#P-255) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information