NBQX (2,3-dioxo-6-nitro-7-sulfamoyl-benzo
uinoxaline) is an
antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
of the
AMPA receptor
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic receptor, ionotropic transmembrane receptor for glutamate (iGluR) that mediates fast synapse, synap ...
.
NBQX blocks AMPA receptors in micromolar concentrations (~10–20 μM) and also blocks
kainate receptor
Kainate receptors, or kainic acid receptors (KARs), are ionotropic receptors that respond to the neurotransmitter glutamate. They were first identified as a distinct receptor type through their selective activation by the agonist kainate, a drug ...
s. In experiments, it is used to counter
glutamate
Glutamic acid (symbol Glu or E; the ionic form is known as glutamate) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can syn ...
excitotoxicity
In excitotoxicity, nerve cells suffer damage or death when the levels of otherwise necessary and safe neurotransmitters such as glutamate become pathologically high, resulting in excessive stimulation of receptors. For example, when glutamate re ...
. NBQX was found to have anticonvulsant activity in rodent seizure models.
[Yamaguchi, S.; Donevan, S.D.; Rogawski, M.A. (1993). Anticonvulsant activity of AMPA/kainate antagonists: comparison of GYKI 52466 and NBOX in maximal electroshock and chemoconvulsant seizure models. ''Epilepsy Res.'' 15:179–184.]
As the disodium salt, NBQX is soluble in water at high concentrations (at least up to 100 mM).
See also
*
CNQX
CNQX or cyanquixaline (6-cyano-7-nitroquinoxaline-2,3-dione) is a competitive AMPA/kainate receptor antagonist. Its chemical formula is C9H4N4O4. CNQX is often used in the retina to block the responses of OFF-bipolar cells for electrophysiology ...
*
DNQX
DNQX (6,7-dinitroquinoxaline-2,3-dione) is a competitive antagonist at AMPA and kainate receptor antagonist, receptors, two ionotropic glutamate receptor (iGluR) subfamilies. It is used in a variety of molecular biology subfields, notably neurophy ...
*
Fanapanel
Fanapanel (INN, code name ZK-200775), also known as MPQX, is a quinoxalinedione derivative drug which acts as a competitive antagonist of the AMPA receptor. It was under development by Schering AG for the treatment of cerebral ischemia associat ...
(MPQX)
*
Quinoxalinedione
Quinoxalinedione is an organic compound with the formula C6H4(NH)2(CO)2. It is a colorless solid that is soluble in polar organic solvents. Quinoxalinediones are a family of related compounds sharing the same bicyclic core. Various quinoxalinedi ...
References
AMPA receptor antagonists
Kainate receptor antagonists
Glycine receptor antagonists
Sulfonamides
Nitronaphthalenes
Quinoxalines
Lactams
Quinones
Nitrogen heterocycles
{{biochem-stub