CIQ

3-chlorophenyl)(6,7-dimethoxy-1-((4-methoxyphenoxy)methyl)-3,4-dihydroisoquinolin-2(1 H)-yl)methanone
A Selective Potentiator of GluN2C/GluN2D-Containing NMDA Receptors
  • New
Cat #: C-275
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 467.95
    Purity: >99% (HPLC)
    Effective concentration 1-20 µM.
    Structure
    Chemical name (3-chlorophenyl)-[6,7-dimethoxy-1-[(4-methoxyphenoxy)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone
    Molecular formula C26H26ClNO5
    CAS No.: 486427-17-2.
    Activity CIQ is an NR2C and NR2D selective potentiator of NMDA receptors. It enhances receptor responses two-fold with EC50 of 3 µM by increasing channel opening frequency1.
    References - Activity
    1. Mullasseril, P. et al. (2010) Nat. Commun. 1, 90.
    Storage before reconstitution 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.
    Reconstitution Soluble in DMSO up to 100 mM.
    Centrifuge all products before handling (10000 x g 5 min).
    Storage after reconstitution Store at -20°C.
    It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    Alomone Labs CIQ potentiates NMDA receptors expressed in Xenopus oocytes.
    Representative time course of NR1/NR2C currents, elicited by transient stimulations with 100 µM glutamate + 40 µM glycine every 50 sec, while membrane potential was held at -80 mV, and significantly enhanced by 5 µM CIQ (#C-275).
    References - Scientific Background
    1. Mullasseril, P. et al. (2010) Nat. Commun. 1, 90.
    2. Suryavanshi, P.S. et al. (2014) Br. J. Pharmacol. 171, 799.
    3. Black, S.A. et al. (2014) Front. Cell Dev. Biol. 2, 45.
    Scientific background

    CIQ is a positive allosteric potentiator selective for NR2C- and NR2D-containing N-methyl-d-aspartate (NMDA) receptors. The compound does not potentiate other NMDA receptor subtypes or AMPA and Kainate receptors. The activity of CIQ depends on a single residue in the M1 region of the receptor1,2. CIQ demonstrates potentiating EC50 values of 2.7 and 2.8 μM, for NR2C- and NR2D-containing receptors respectively1.

    NMDA receptors are tetrameric entities composed of two obligatory GluN1 and two GluN2 subunits. They play important roles in numerous cellular processes and brain functions such as synaptic plasticity, addiction, and stroke. NMDA receptors also mediate physiological functions such as learning and memory formation. They are also involved in many neurodegenerative conditions including Alzheimer’s disease2,3.

    Target NMDA receptors

    Check out more of our new products.

    Last update: 22/11/2018

    CIQ (#C-275) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use