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CNS-1102

Cerestat, Aptiganel hydrochloride
A Potent NMDA Receptor Antagonist
Cat #: C-305
Alternative Name Cerestat, Aptiganel hydrochloride
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 339.86
    Purity: >99%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name 1-(3-ethylphenyl)-1-methyl-2-naphthalen-1-ylguanidine hydrochloride.
    Molecular formula C20H22ClN3.
    CAS No.: 137160-11-3.
    PubChem CID 60839
    Activity CNS-1102 is a potent, use-dependent, non-competitive blocker of NMDA receptors, exhibiting high affinity for the central ion channel site (IC50 = 36 nM versus [3H]-MK-801)1.
    References-Activity
    1. Reddy, N.L. et al. (1994) J. Med. Chem. 37, 260.
    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 100 mM in DMSO and to 50 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs CNS-1102 inhibits NMDA receptor channels expressed in Xenopus oocytes.
      Alomone Labs CNS-1102 inhibits NMDA receptor channels expressed in Xenopus oocytes.
      A. Time course of NR1/NR2A currents elicited by transient stimulations with 100 µM glutamate and 100 µM glycine every 100s, while membrane potential was held at -80 mV. Application of 200 nM CNS-1102 (#C-305) for 10 min (green) significantly inhibits current amplitude. B. Superimposed current traces from the recording shown in A upon application of control (black) and of 200 nM CNS-1102 (green).
    References - Scientific background
    1. Schäbitz, W.R. et al. (2000) Stroke 31, 1709.
    2. Albers, G.W. et al. (2001) JAMA. 286, 2673.
    3. Black, S.A. et al. (2014) Front. Cell Dev. Biol. 2, 45.
    Scientific background

    CNS-1102 is a potent, non-competitive, and selective NMDA receptor (N-methyl-D-aspartate) antagonist. In animals, CNS-1102 reduces the volume of ischemic cerebral infarction and in humans it is being used as a potential agent for the treatment of acute ischemic stroke or neurotrauma stroke. It has the ability to protect white and gray matter from ischemic injury1,2.

    NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. NMDAR plays an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. They also mediate physiological functions such as learning and memory formation, glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease3.

    Target NMDA receptors
    Last update: 23/08/2020

    CNS-1102 (#C-305) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
    Product citations
    1. Amakhin, D.V. et al. (2018) Front. Cell. Neurosci. 12, 486.
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