| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Disodium salt DNQX (FG 9041) selectively depolarizes neurons in the thalamic reticular nucleus (TRN) [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] |
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| ln Vivo |
A particular AMPA receptor antagonist called DNQX (FG 9041) dramatically lowers the amount of phencyclidine administered intraperitoneally (5 μl 0.5 mg/ml) or subcutaneously (10 mg/kg) at 5 mg/kg or 10 mg/kg. In the posterior cingulate and retrosplenial cortex, PCP (40 mg/kg) and ketamine (80, 100, 120 mg/kg) cause hsp70 to be induced [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 |
The N-methyl-D-aspartate (NMDA)-subtype of glutamate receptors has been well described as a result of the early appearance of NMDA antagonists, but no potent antagonist for the "non-NMDA" glutamate receptors has been available. Quinoxalinediones have now been found to be potent and competitive antagonists at non-NMDA glutamate receptors. These compounds will be useful in the determination of the structure-activity relations of quisqualate and kainate receptors and the role of such receptors in synaptic transmission in the mammalian brain.[1]
|
| Molecular Formula |
C8H2N4NA2O6
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|---|---|
| Molecular Weight |
296.104222774506
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| Exact Mass |
295.976
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| Elemental Analysis |
C, 32.45; H, 0.68; N, 18.92; Na, 15.53; O, 32.42
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| CAS # |
1312992-24-7
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| Related CAS # |
DNQX;2379-57-9
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| PubChem CID |
45073428
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.13
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Na+].[Na+].O=[N+](C1=CC2=NC(=C(N=C2C=C1[N+]([O-])=O)[O-])[O-])[O-]
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| InChi Key |
GPSBSOYURFUVKJ-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C8H4N4O6.2Na/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);;/q;2*+1/p-2
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| Chemical Name |
disodium;6,7-dinitroquinoxaline-2,3-diolate
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| Synonyms |
DNQX 2Na; DNQXDisodiumSalt; DNQX DISODIUM; 6,7-Dinitroquinoxaline-2,3-dione disodium salt; DNQX disodium salt?; disodium;6,7-dinitroquinoxaline-2,3-diolate; C8H2N4Na2O6;DNQX Disodium
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3772 mL | 16.8862 mL | 33.7724 mL | |
| 5 mM | 0.6754 mL | 3.3772 mL | 6.7545 mL | |
| 10 mM | 0.3377 mL | 1.6886 mL | 3.3772 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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