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 K_i of 0.59 μM. 7-Chlorokynurenic acid has potent antinociceptive actions after neuraxial delivery^[1][2]. IC50 & Target: Ki: 0.59 μM (reuptake of glutamate)^[1]
IC50: 0.56 μM (Glycine B coagonist site of NMDA receptor)^[2] 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].