Overview
- Traynelis, S.F. et al. (2010) Pharmacol. Rev. 62, 405.
Alomone Labs NBQX disodium salt inhibits GluA1 channels expressed in Xenopus oocytes.Representative time course of GluA1 current, activated by a continuous application (top dotted line) of 10 µM glutamate, and reversibly inhibited by 5 µM NBQX disodium salt (#N-186), as indicated (horizontal bar), at a holding potential of -60 mV.
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) is a non-N-methyl-D-aspartate (non-NMDA) type ionotropic transmembrane receptor for glutamate that mediates fast synaptic transmission in the central nervous system (CNS)1. AMPA receptors normally assemble from four genetically distinct subunits: GluR1, GluR2, GluR3, and GluR4, which combine to form receptor complexes with different functional properties2.
NBQX (2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F) quinoxaline) is an analogue of the quinoxalinedione antagonists to the non-NMDA glutamate receptor. NBQX is a potent and selective inhibitor of binding to the quisqualate subtype of the glutamate receptor, with no activity at the NMDA and glycine site3. It is a specific and potent AMPA receptor antagonist and has been found to be neuroprotective in various models of ischemia and to have anticonvulsant properties in different models of epilepsy4. NBQX has been reported to block the excitatory actions of AMPA in rat neocortex slices while having no effect on NMDA responses5. It was also reported to selectively block AMPA-induced depolarizations but not spontaneous epileptiform discharges in Mg2+ free medium in the rat cortical wedge6. NBQX blocks AMPA and kainate receptors at micromolar concentrations7,8.
