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7-Chlorokynurenic acid

7-CKA, 7-CTKA

An Antagonist of NMDA Receptors

Cat #: C-285
Alternative Name 7-CKA, 7-CTKA
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 223.61
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
    Structure
    Chemical name 7-chloro-4-oxo-1H-quinoline-2-carboxylic acid.
    Molecular formula C10H6ClNO3.
    CAS No.: 18000-24-3
    PubChem CID 1884
    Activity 7-Chlorokynurenic acid is an NMDA receptor antagonist that acts at the glycine site with IC50 of 3.4 μM1.
    References-Activity
    1. Green, T. et al. (2002) Mol. Pharmacol. 61, 326.
    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 DMSO. 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 7-Chlorokynurenic acid inhibits NMDA (NR1+NR2A) receptors expressed in Xenopus oocytes. 
      Alomone Labs 7-Chlorokynurenic acid inhibits NMDA (NR1+NR2A) receptors expressed in Xenopus oocytes. 
      A. Time course of NMDA currents elicited with 10 µM glutamate and 10 µM glycine every 50 sec, while membrane potential was held at -80 mV. 20 µM 7-Chlorokynurenic acid (#C-285), 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. Green, T. et al. (2002) Mol. Pharmacol. 61, 326.
    2. Zhu, W.L. et al. (2013) J. Psychiatry. Neurosci. 38, 306.
    3. Wu, H.Q. et al. (2005) Epilepsia 46, 1010.
    4. Black, S.A. et al. (2014) Front. Cell. Dev. Biol. 2, 45.
    5. Kemp, J.A. et al. (1988) Proc. Natl. Acad. Sci. U.S.A. 85, 6547.
    Scientific background

    7-Chlorokynurenic acid (7-CKA), a derivative of kynurenic acid, is a potent and selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. 7-CKA acts and binds with high affinity to the glycine binding site located on the NMDA receptor. This compound has neuroprotective, antinociceptive and anticonvulsive effects lacking the ability to penetrate the blood-brain-barrier and has therapeutic potential in some types of epilepsy1-3. Several studies that conducted radioligand binding experiments showed that 7-chlorokynurenic acid binds to the strychnine-glycine binding site with high affinity (IC50 value of 0.56 μM)5.

    Several studies have shown that acute administration of 7-CKA can produce rapid antidepressant-like effects without showing addictive potential2. It seems that inhibition of the phospho-glycogen synthase kinase-3β pathway and activation of the mammalian target of rapamycin in the medial prefrontal cortex are connected to the 7-CKA rapid behavioural response2.

    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 disease4.

    Target NMDA receptors
    Last update: 25/07/2021

    7-Chlorokynurenic acid (#C-285) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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