Arcaine sulfate

An Antagonist of NMDA Receptors
    Cat #: A-285
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 270.31
    Purity: >95%
    Form Lyophilized powder.
    Effective concentration 50-500 µM.
    Structure
    • Arcaine sulfate
    Chemical name 2-[4-(diaminomethylideneamino)butyl]guanidine;sulfuric acid.
    Molecular formula C6H18N6O4S.
    CAS No.: 14923-17-2.
    PubChem CID 119020
    Activity Arcane is an NMDA receptor antagonist with KD of 61 µM at -60 mV1.
    References-Activity
    1. Donevan, S.D. et al. (1992) Mol. Pharmacol. 41, 727.
    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 20 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
    • Arcaine sulfate
      Alomone Labs Arcaine sulfate inhibits NMDA (NR1+NR2A) channels expressed in Xenopus oocytes. 
      A. Time course of NMDA currents elicited with 10 µM glutamate and 10 µM glycine, every 50s, while membrane potential was held at -60 mV. 200 µM Arcaine sulfate (#A-285) applied for 5min, as indicated, partially inhibited current amplitude. B. Superimposed current traces taken from the experiment described in A.
    References - Scientific background
    1. Donevan, S.D. et al. (1992) Mol. Pharmacol. 41, 727.
    Scientific background

    Glutamate is the main excitatory neurotransmitter in the CNS and is also involved in a variety of pathological conditions including epilepsy. Glutamate binds to the ionotropic NMDA receptor to relay its excitatory signal.

    Arcaine sulfate is a competitive inhibitor of the NMDA receptor and also an inhibitor of the enzyme NO synthase. It has an effective concentration of 50-500 µM and an IC50 of 61 μM at -60 mV. Arcaine binds to the polyamine recognition site of the NMDA receptor complex and blocks the receptor in a concentration- and voltage-dependent manner. At positive membrane potentials Arcaine does not produce a blocking effect. In the presence of 100 μM Arcaine (at -60 mV), NMDA amplitude whole cell currents are reduced by 67% and by 69% in single channel recordings. The inhibitory effect of Arcaine is rapid in onset and recovery (<100 ms in both cases) and occurs when the receptor is in its open state. Arcaine does not inhibit other glutamate receptors such as AMPA and kainate and does not affect GABA elicited currents. When applied with dizocilpine, another open state NMDA blocker, Arcaine prevents dizocilpine from producing a long lasting blockade of the receptor thus indicating the existence of a competitive interaction between the two substances1.

    Target NMDA receptors
    Last update: 24/01/2020

    Arcaine sulfate (#A-285) 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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