DNQX disodium salt

Non Antibodies

AMPA/kainate receptors

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

296, 1

AMPA/Kainate Receptor Antagonist

Centrifuge the vial before adding solvent (10, 000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. For long-term storage of diluted solutions, we recommend adding 0.1% BSA. Repeat freeze-thawing may result in loss of activity.

41116134

AMPA/kinate receptor antagonists. Association of AMPA receptors with TARPs converts DNQX from antagonist to weak partial agonist1. The concentration that inhibits 50% of AMPA binding (IC50) for DNQX is 0.50 ± 0.10 µM, and is about one-fifth as effective at kainate binding sites, 2.0 ± 0.1 uM in rat cortical membranes2. The IC50 of DNQX is 1 µM in a crystal structure of the GluR2 ligand binding core3.

Yes

The first widely used competitive AMPA receptor antagonists were quinoxalinediones (CNQX, DNQX, NBQX), which were highly selective over NMDA receptors but antagonized kainate receptors. Surprisingly, association of AMPA receptors with TARP auxiliary subunits converts DNQX from an antagonist to a weak partial agonist. DNQX induces partial domain closure, consistent with the activity of a partial agonist. DNQX interacts with residues primarily within domain D1 of the clamshell, thereby depriving the agonist of its initial contact sites with the open cleft of the binding pocket1.The concentrations that inhibit 50% of AMPA binding (IC50) for DNQX is 0.50 ± 0.10 µM, and about one-fifth as effective at kainate binding sites, 2.0 ± 0.1 µM in rat cortical membranes2. The IC50 of DNQX is 1 µM in a crystal structure of the GluR2 ligand binding core3.