| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
non-NMDA glutamate receptor; Kainate Receptor
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|---|---|
| ln Vitro |
Thalamic reticular nucleus (TRN) neurons are selectively depolarized by DNQX [2].
The quinoxaline derivative 6,7-dinitroquinoxaline-2,3-dione (DNQX) selectively depolarizes thalamic reticular nucleus (TRN) neurons. A: DNQX (20 μM) produces a reversible membrane depolarization in a TRN neuron. In contrast, DNQX (20 μM) application does not alter the membrane potential in a ventrobasal (VB) neuron. The transient downward deflections, in this and following figures, are membrane responses to short hyperpolarizing current steps. Graph depicts population data illustrating differential effect of DNQX. B: in a voltage-clamped TRN neuron (Vhold = −70mV), DNQX (20 μM) produces a reversible inward current. DNQX does not alter the holding current of a VB neuron. C: in a different TRN neuron, a lower DNQX concentration (4 μM) produces no change in membrane potential, whereas at a higher concentration, DNQX (100 μM) produces a robust depolarization. Plot illustrates concentration-dependent effects of DNQX on membrane potential of TRN neurons. D: the DNQX-mediated depolarizations persist in TTX (0.5 μM) or a low Ca2+ (0.2 mM)/high Mg2+ (6 mM)-containing physiological solution. [2] |
| ln Vivo |
DNQX is a particular AMPA receptor antagonist that considerably lowers the amount of phencyclidine (PCP) that is induced in the posterior cingulate and retrosplenial cortex by 5 mg/kg or 10 mg/kg intraperitoneally or intracerebroventricularly (5 μl, 0.5 mg/ml) (40 mg/kg) and ketamine (80, 100, 120 mg/kg) [3].
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| Cell Assay |
Quinoxaline derivatives [e.g., 6,7-dinitroquinoxaline-2,3-dione (DNQX), 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX)] have routinely been used as non-NMDA receptor antagonists over the last two decades. In this study, we examined whether quinoxaline derivatives alter the intrinsic properties of thalamic neurons in light of recent findings indicating that these compounds can alter neuronal excitability in hippocampal and cerebellar neurons via transmembrane AMPA receptor (AMPAR) regulatory proteins (TARPs). Whole cell recordings were obtained from TRN and ventrobasal (VB) thalamic relay neurons in vitro. DNQX and CNQX produced a consistent depolarization in all TRN neurons tested. The depolarization persisted in tetrodotoxin and low Ca²+/high Mg²+ conditions, suggesting a postsynaptic site of action. In contrast, DNQX and CNQX produced little or no change in VB thalamocortical relay neurons. The nonspecific ionotropic glutamate receptor antagonist, kynurenic acid, and the selective AMPAR antagonist, 4-(8-methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine hydrochloride, blocked the DNQX-mediated depolarizations. Our results indicate that the DNQX- and CNQX-mediated depolarizations are mediated by AMPAR but not kainate receptors in TRN neurons. The AMPAR-positive allosteric modulator, trichloromethiazide, potentiated the DNQX-mediated depolarization in TRN neurons but did not unmask any excitatory actions of DNQX/CNQX in relay neurons. This selective action may not only reveal a differential TARP distribution among thalamic neurons but also may provide insight into distinct characteristics of AMPA receptors of thalamic neurons that could be exploited by future pharmacological development. Furthermore, these data suggest that quinoxaline derivatives could modulate synaptic transmission and alter neuronal excitability[2].
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| Animal Protocol |
The present study shows that DNQX, a specific AMPA receptor antagonist, given as either a 5 mg/kg or 10 mg/kg intraperitoneal dose or into the lateral cerebral ventricle (5 microliters of 0.5 mg/ml) significantly diminished PCP (40 mg/kg) and ketamine (80, 100, 120 mg/kg) hsp70 induction in the posterior cingulate and retrosplenial cortex. The most dramatic decrease of hsp70 induction was seen with the intraventricular dose of DNQX. Present findings show that the AMPA receptor has a role in PCP/ketamine induction of hsp70 in the cortex. DNQX inhibition of PCP/ketamine hsp70 induction was likely related to AMPA receptor antagonism which prevented excess calcium influx via voltage-gated calcium channels.[3]
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| References |
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| Additional Infomation |
6,7-dinitro-1,4-dihydroquinoxaline-2,3-dione is a quinoxaline derivative.
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| Molecular Formula |
C8H4N4O6
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|---|---|
| Molecular Weight |
252.1406
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| Exact Mass |
252.013
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| Elemental Analysis |
C, 38.11; H, 1.60; N, 22.22; O, 38.07
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| CAS # |
2379-57-9
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| Related CAS # |
DNQX disodium salt;1312992-24-7
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| PubChem CID |
3899541
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
670.7ºC at 760 mmHg
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| Melting Point |
>300°C
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| Flash Point |
359.4ºC
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| Vapour Pressure |
1.33E-18mmHg at 25°C
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| Index of Refraction |
1.665
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| LogP |
1.13
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
386
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RWVIMCIPOAXUDG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H4N4O6/c13-7-8(14)10-4-2-6(12(17)18)5(11(15)16)1-3(4)9-7/h1-2H,(H,9,13)(H,10,14)
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| Chemical Name |
6,7-dinitro-1,4-dihydroquinoxaline-2,3-dione
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| Synonyms |
dnqx; 2379-57-9; 6,7-dinitro-1,4-dihydroquinoxaline-2,3-dione; FG-9041; 6,7-Dinitroquinoxaline-2,3(1H,4H)-dione; 6,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione; 6,7-Dinitroquinoxaline-2,3-dione (DNQX); 2,3-Quinoxalinedione, 1,4-dihydro-6,7-dinitro-;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 35 mg/mL (~138.81 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (8.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9661 mL | 19.8303 mL | 39.6605 mL | |
| 5 mM | 0.7932 mL | 3.9661 mL | 7.9321 mL | |
| 10 mM | 0.3966 mL | 1.9830 mL | 3.9661 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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