7-Chloro-4-hydroxyquinoline-2-carboxylic acid (7-Chlorokynurenic acid) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chloro-4-hydroxyquinoline-2-carboxylic acid is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chloro-4-hydroxyquinoline-2-carboxylic acid has potent antinociceptive actions after neuraxial delivery[1][2].
Male Sprague-Dawley rats pretreated with 7-Chloro-4-hydroxyquinoline-2-carboxylic 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[3].
References:
[1]. Kemp JA, et al. 7-Chlorokynurenic acid is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex. Proc Natl Acad Sci U S A. 1988 Sep;85(17):6547-50.
[2]. Yaksh TL, et al. Characterization of the Effects of L-4-Chlorokynurenine on Nociception in Rodents. J Pain. 2017 Oct;18(10):1184-1196.
[3]. Croucher MJ, et al. 7-Chlorokynurenic acid, a strychnine-insensitive glycine receptor antagonist, inhibits limbic seizurekindling. Neurosci Lett. 1990 Oct 2;118(1):29-32.