Target
Ki: 0.59 μM (reuptake of glutamate)
IC50: 0.56 μM (Glycine B coagonist site of NMDA receptor)
Uses
NMDA receptor antagonist at the glycine site
Definition
ChEBI: A quinolinemonocarboxylic acid that is quinaldic acid which is substituted by a hydroxy group at position 4 and by a chlorine at position 7. It is a potent NMDA glutamate receptor antagonist which antagonizes the strychnine-insensitive glycine site of the
MDA receptor. It also prevents neurodegeneration produced by quinolinic acid.
Biological Functions
Glycine B agonist site antagonist of N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid is also a potent inhibitor of glutamate reuptake into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid has potent analgesic effects in neurotransmission.
Biological Activity
NMDA receptor antagonist acting at the glycine site. Potent competitive inhibitor of L-glutamate transport into synaptic vesicles. Also available as part of the NMDA Receptor - Glycine Site Tocriset™ .
in vivo
Male Sprague-Dawley rats pretreated with 7-Chlorokynurenic acid (10 nM) shows a significant retardation of development of both the electroencephalographic and motor (17.7±2.9 daily stimulations) components of the seizure response.
