5,7-Dichlorokynurenic Acid

5,7-Dichlorokyneurenic acid (5,7-DCKA) is a derivative of kynurenic acid (Item No. 16792) and an NMDA receptor antagonist (K_i = 40 nM in a radioligand binding assay).¹ It selectively inhibits glycine- over kainate-induced NMDA currents at 15 μM in Xenopus oocytes expressing rat NMDA receptors. 5,7-DCKA reduces NMDA-induced neurotoxicity in primary rat cortical neurons by 55 to 90% when used at concentrations ranging from 1 to 10 μM. In vivo, 5,7-DCKA (0.97-97 nmol) reverses mechanical hyperalgesia in magnesium-deficient rats in a dose-dependent manner.² It blocks the positive ionotropic effect, hypertension, and increase in myocardial oxygen demand induced by electrical stimulation of the paraventricular nucleus (PVN) in anesthetized rabbits.³ 5,7-DCKA also increases social interaction time in the social interaction test and time spent in the open arms of the elevated plus maze, indicating anxiolytic-like activity, as well as disinhibits conflict responding in the Cook and Davidson conditioned conflict paradigm.⁴

WARNING This product is not for human or veterinary use.

1. McNamara, D.J., Smith, E.C.R., Calligaro, D.O., et al. 5,7-Dichlorokynurenic acid, a potent and selective competitive antagonist of the glycine site on NMDA receptors. Neurosci. Lett. 120(1), 17-20 (1990).

2. Begon, S., Pickering, G., Eschalier, A., et al. Role of spinal NMDA receptors, protein kinase C and nitric oxide synthase in the hyperalgesia induced by magnesium deficiency in rats. Br. J. Pharmacol. 134(6), 1227-1236 (2001).

3. Monassier, L., Tibiriça, E., Roegel, J.-C., et al. Prevention by NMDA receptor antagonists of the centrally-evoked increases of cardiac inotropic responses in rabbits. Br. J. Pharmacol. 111(4), 1347-1354 (1994).

4. Corbett, R., and Dunn, R.W. Effects of 5,7 dichlorokynurenic acid on conflict, social interaction and plus maze behaviors. Neuropharmacology 32(5), 461-466 (1993).