NBQX

NBQX is a highly selective and competitive AMPA receptor antagonist.

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

AMPA receptor[1]

NBQX has a high affinity for AMPA and kainate binding sites with little or no affinity for the glutamate recognition site on the NMDA receptor complex[1].

NBQX is neuroprotective in a focal ischaemia model in the rat when given as an i.v. bolus dose of 30 mg/kg at the time of MCA occlusion and again at 1 h post occlusion[1]. NBQX provides potent anticonvulsant protection against AMPA. The ED50 values for the protection against AMPA-induced seizures by NBQX (30 min, i.p.) is 23.6 (11.6- 48.0)[2].

Rats[1] Male Sprague-Dawley rats weighing 350-390 g are used for study. 30 mg/kg of NBQX (2x15 mg/mL) is administered i.v. as a bolus dose followed by an infusion of 10 mg/kg/h for 4 h, the bolus dose and infusion are started immediately after MCA occlusion. Blood samples are taken from these animals at 1, 2, 3 and 4 h after the start of the infusion and the plasma level of NBQX in each sample is measured[1]. Mice[1] The time course for the anticonvulsant action of NBQX and of GYKI 52466 against AMPA-induced seizures is determined by pretreating groups (n=10) of Swiss mice with 30 and 60/zmol/kg NBQX or GYKI 52466 (i.p.) 15-120 min before challenging the mice with a convulsant dose of AMPA (5 nmol) i.c.v[2].

[1]. Fukushima K, et al. Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to Physiologically Relevant Assays for Multiple Ionotropic Glutamate Receptors. J Biomol Screen. 2014 Sep; 19(8):1174-84.

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