Bioactivity | 7-Chlorokynurenic acid (7-CKA) 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-Chlorokynurenic acid is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid has potent antinociceptive actions after neuraxial delivery[1][2]. | ||||||||||||
Target | Ki: 0.59 μM (reuptake of glutamate)IC50: 0.56 μM (Glycine B coagonist site of NMDA receptor) | ||||||||||||
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[3]. | ||||||||||||
Name | 7-Chlorokynurenic acid | ||||||||||||
CAS | 18000-24-3 | ||||||||||||
Formula | C10H6ClNO3 | ||||||||||||
Molar Mass | 223.61 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |