The NBQX Story

Publisher Summary This chapter discusses pharmacology of 2,3-dihydroxy-6-nitro-7-sulfamoylbenzo[f]quinoxaline (NBQX). NBQX is the first selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonist to demonstrate neuroprotective properties in animal models of focal and global cerebral ischemia. NBQX potently increased the focal seizure threshold and inhibited seizure spread from the focus. It protected against seizure induced by maximal electroshock (MES) and pentylenetetrazol. NBQX treatment did not reverse the Parkinsonism nor changed the responses to the selective D 2 dopamine receptor agonist (+)-PHNO or the partial dopamine D 1 receptor agonist CY208-243 in two Parkinsonian monkeys. NBQX can reduce the hippocampal CA1 neuronal loss observed following severe cerebral trauma, suggesting a further potential clinical use for AMPA antagonists in head injury. It is suggested that NBQX be administered in relatively high doses to get an anti-ischemic effect. It is observed that NBQX is as efficacious as the N -methyl- D -aspartate (NMDA) antagonists in most models of focal ischemia and does not seem to have the psychotomimetic side-effect problem.