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CNQX disodium

Names

[ CAS No. ]:
479347-85-8

[ Name ]:
CNQX disodium

[Synonym ]:
Disodium 6-cyano-7-nitro-2,3-quinoxalinediolate
disodium 6-cyano-7-nitroquinoxaline-2,3-diolate
6-Quinoxalinecarbonitrile, 1,2,3,4-tetrahydro-7-nitro-2,3-dioxo-, sodium salt (1:2)

Biological Activity

[Description]:

CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist[1]. CNQX disodium blocks the expression of fear-potentiated startle in rats[5].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR
Research Areas >> Neurological Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[Target]

IC50: 0.3 μM (AMPA) and 1.5 μM (kainate receptor)[1]


[In Vitro]

CNQX disodium (FG9065 disodium; 2-5 μM) reversibly blocks the Schaffer collateral and mossy fibre excitatory postsynaptic potential (EPSP), while sparing the fast and slow GABA-mediated inhibition in superfusion of hippocampal slices[2]. CNQX disodium (1-5 μM) produces a selective and dose-dependent reduction in the amplitude of the monosynaptic component of the DR-VRR recorded from lumbar spinal segments[3].

[In Vivo]

CNQX disodium (FG9065 disodium; 0.75-3 mg/kg; IP; 20 min before testing) decreased the number of cocaine responses in a dose-dependent manner during the first 15-min cocaine-free interval[4]. The bilateral infusion of CNQX disodium (0.5 or 1.25 μg) into the amygdala or dorsal hippocampus 10 min prior to a retention test partially blocks the expression of stepdown inhibitory avoidance in rats 24 h after training. CNQX disodium causes a complete blockade at a dose of 0.5 μg[5]. Animal Model: Male Wistar rats weighing 180-200 g[4] Dosage: 0.75, 1.5, and 3 mg/kg Administration: IP; 20 min before testing Result: Decreased the number of cocaine (IV; 0.25 mg/infusion) responses in a dose-dependent manner during the first 15-min cocaine-free interval.

[References]

[1]. T Honoré, et al. Quinoxalinediones: Potent Competitive non-NMDA Glutamate Receptor Antagonists. Science. 1988 Aug 5;241(4866):701-3.

[2]. Neuman RS, et al. Blockade of excitatory synaptic transmission by 6-cyano-7-nitroquinoxaline-2,3-dione(CNQX) in the hippocampus in vitro. Neurosci Lett. 1988 Sep 23;92(1):64-8.

[3]. Alford S, et al. CNQX and DNQX block non-NMDA synaptic transmission but not NMDA-evoked locomotion in lamprey spinal cord. Brain Res. 1990 Jan 8;506(2):297-302.

[4]. Pia Bäckström, et al. Attenuation of Cocaine-Seeking Behaviour by the AMPA/kainate Receptor Antagonist CNQX in Rats. Psychopharmacology (Berl). 2003 Feb;166(1):69-76.

[5]. Kim M, et al. Infusion of the non-NMDA receptor antagonist CNQX into the amygdala blocks the expression of fear-potentiated startle. Behav Neural Biol. 1993 Jan;59(1):5-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C9H2N4Na2O4

[ Molecular Weight ]:
276.116

[ Exact Mass ]:
275.987152


Related Compounds