TCN 201

QCR-22
An Antagonist of NMDA Receptors
    Cat #: T-190
    Alternative Name QCR-22
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 461.89
    Purity: >98%
    Effective concentration 0.1-10 µM.
    Structure
    • TCN 201
    Chemical name N-[[4-(benzamidocarbamoyl)phenyl]methyl]-3-chloro-4-fluorobenzenesulfonamide.
    Molecular formula C21H17ClFN3O4S.
    CAS No.: 852918-02-6.
    PubChem CID 4787937
    Activity TCN 201 blocks NR1/NR2A NMDA receptors in an NR1 co-agonist dependent and non-competitive manner1, selective for NR2A- over NR2B-containing receptors, with pIC50 of 6.8 on human recombinant NR1/NR2A in FLIPR/Ca2+ assay2.
    References-Activity
    1. Edman, S. et al. (2012) Neuropharmacology 63, 441.
    2. Bettini, E. et al. (2010) J. Pharmacol. Exp. Ther. 335, 636.
    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 100mM in DMSO. 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
    • TCN 201
      Alomone Labs TCN 201 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 100 sec, while membrane potential was held at -80 mV. Application of 1 µM TCN 201 (#T-190) for 5 min (green), significantly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control (black) and of 1 µM TCN 201 (green).
    References - Scientific background
    1. Edman, S. et al. (2012) Neuropharmacology 63, 441.
    2. Black, S.A. et al. (2014) Front. Cell. Dev. Biol. 2, 45.
    Scientific background

    TCN 201, a sulphonamide derivative, acts as a selective and potent NMDA (methyl-D-aspartate) receptor antagonist. This compound displays a high selectivity for GluN1/GluN2A-containing NMDAR receptors over GluN1/GluN2B containing receptors and acts in a non-competitive manner. The degree of its antagonism is dependent on the concentration of the GluN1-site co-agonist, glycine or D-serine, and is independent of the glutamate concentration1. TCN 201 can be used to estimate and to clarify the contribution of NMDAR subunit and its composition and function.

    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. NMDA receptors mediate physiological functions such as learning and memory formation. They play a role in glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease2.

    Target NMDA receptors
    Last update: 24/01/2020

    TCN 201 (#T-190) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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