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NBQX disodium salt

Catalog No.GC13482

NBQX disodium salt (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist.

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NBQX disodium salt Chemical Structure

Cas No.: 479347-86-9

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

HIP-009 cells

Preparation Method

Assessed the effects of NBQX disodium salt and CNQX—antagonists of AMPARs and KARs—on the AMPA- or KA-evoked calcium rise to confirm the functions of these receptors in differentiated HIP-009 cells.

Reaction Conditions

30 µM NBQX disodium salt

Applications

NBQX disodium salt inhibited both AMPA or kainic acid (KA) induced signals in a concentration-dependent manner, with IC50 values being 0.7 ± 0.1 and 0.7 ± 0.03 µM, respectively. The AMPA-evoked calcium rise was completely inhibited by NBQX disodium salt, whereas 68.6% ± 1.3% inhibition of the KA-induced signal was observed with 30 µM of NBQX disodium salt treatment.

Animal experiment [2]:

Animal models

Male Wistar rats

Preparation Method

To observe anti-epileptic effects of NBQX disodium salt in PTZ induced epilepsy,rats into four groups: rats in saline + saline group were treated with saline only; rats in PTZ + saline group were treated with 50 mg/kg of PTZ and saline for 28 days; rats in saline + NBQX disodium salt group were treated with saline for 28 days, and 20 mg/kg of NBQX disodium salt for next 3 days; rats in PTZ + NBQX disodium salt group were treated with 50 mg/kg of PTZ for 28 days and were treated with 20 mg/kg of NBQX disodium salt for next 3 days. Behavioral tests and neurochemical analysis were performed on the following 2 days.

Dosage form

20 mg/kg NBQX disodium salt Once daily by intraperitoneal injection for 3 days

Applications

NBQX disodium salt was sufficient to decrease pentylenetetrazole-induced seizures through increasing the latency to seizures, decrease the duration of seizure onset, and reduce the scores for the severity of seizures.

References:

[1]: Fukushima K, Tabata Y, et,al.Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to Physiologically Relevant Assays for Multiple Ionotropic Glutamate Receptors. J Biomol Screen. 2014 Sep;19(8):1174-84. doi: 10.1177/1087057114541149. Epub 2014 Jun 30. PMID: 24980597.
[2]: Chen W, Li YS, et,al.AMPA Receptor Antagonist NBQX Decreased Seizures by Normalization of Perineuronal Nets. PLoS One. 2016 Nov 23;11(11):e0166672. doi: 10.1371/journal.pone.0166672. PMID: 27880801; PMCID: PMC5120819.

Background

NBQX disodium salt is a potent, highly selective and competitive antagonist of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptors (AMPARs). Inhibition of AMPARs with NBQX disodium salt shows neuroprotective and anticonvulsant activity.

In HIP-009 cells, NBQX disodium salt inhibited both AMPA or kainic acid (KA) induced signals in a concentration-dependent manner, with IC50 values being 0.7 ± 0.1 and 0.7 ± 0.03 µM, respectively. The AMPA-evoked calcium rise was completely inhibited by NBQX disodium salt, whereas 68.6% ± 1.3% inhibition of the KA-induced signal was observed with 30 µM of NBQX disodium salt treatment[1].

NBQX disodium salt had an effect on acute seizure development, resulting in a significantly higher number of mice experiencing seizures, an increase in the number of seizures per mouse, a greater cumulative seizure score per mouse and a significantly higher mortality rate among the mice[6]. NBQX disodium salt was sufficient to decrease pentylenetetrazole-induced seizures through increasing the latency to seizures, decrease the duration of seizure onset, and reduce the scores for the severity of seizures[2]. SRS develop after status epilepticus (SE) induced by intrahippocampal injection of kainate. they were markedly suppressed by NBQX disodium salt and perampanel. However, perampanel was less tolerable than NBQX disodium salt in epileptic mice[3]. In Male Wistar rats,Although NBQX disodium salt did not affect nicotine maintenance, it significantly suppressed the drug-paired responding in the relapse session[4]. Adult male Wistar rats were trained in drinking in dark paradigm (3 weeks), and following stable alcohol intake, ketamine, NBQX disodium salt as well as their combination were injected prior to a 90 min drinking session Both doses of ketamine (5 and 10 mg/kg) and NBQX disodium salt (5 and 10 mg/kg) significantly attenuated percent alcohol intake[5]. In mice lacking NCAM and PSA, NBQX disodium salt-induced ataxia proved to be more intense as compared with wild-type mice. On both mutant backgrounds, NBQX disodium salt significantly elevated seizure thresholds during i.v. infusion of the chemoconvulsant pentylenetetrazole[7].

References:
[1]: Fukushima K, Tabata Y, et,al. Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to Physiologically Relevant Assays for Multiple Ionotropic Glutamate Receptors. J Biomol Screen. 2014 Sep;19(8):1174-84. doi: 10.1177/1087057114541149. Epub 2014 Jun 30. PMID: 24980597.
[2]: Chen W, Li YS, et,al. AMPA Receptor Antagonist NBQX Decreased Seizures by Normalization of Perineuronal Nets. PLoS One. 2016 Nov 23;11(11):e0166672. doi: 10.1371/journal.pone.0166672. PMID: 27880801; PMCID: PMC5120819.
[3]: Twele F, Bankstahl M, et,al.he AMPA receptor antagonist NBQX exerts anti-seizure but not antiepileptogenic effects in the intrahippocampal kainate mouse model of mesial temporal lobe epilepsy. Neuropharmacology. 2015 Aug;95:234-42. doi: 10.1016/j.neuropharm.2015.03.014. Epub 2015 Mar 31. PMID: 25839899.
[4]: Ruda-Kucerova J, Amchova P, et,al. NBQX attenuates relapse of nicotine seeking but not nicotine and methamphetamine self-administration in rats. World J Biol Psychiatry. 2021 Dec;22(10):733-743. doi: 10.1080/15622975.2021.1907714. Epub 2021 Apr 13. PMID: 33787469.
[5]: Ruda-Kucerova J, Babinska Z, et,al.Both ketamine and NBQX attenuate alcohol drinking in male Wistar rats. Neurosci Lett. 2018 Feb 14;666:175-180. doi: 10.1016/j.neulet.2017.12.055. Epub 2017 Dec 28. PMID: 29288725; PMCID: PMC5805612.
[6]: Libbey JE, Hanak TJ, et,al. NBQX, a highly selective competitive antagonist of AMPA and KA ionotropic glutamate receptors, increases seizures and mortality following picornavirus infection. Exp Neurol. 2016 Jun;280:89-96. doi: 10.1016/j.expneurol.2016.04.010. Epub 2016 Apr 9. PMID: 27072529; PMCID: PMC4860063.
[7]: Potschka H, Pekcec A, et,al. Deficiency of neural cell adhesion molecule or its polysialylation modulates pharmacological effects of the AMPA receptor antagonist NBQX. Neuroscience. 2008 Apr 9;152(4):1093-8. doi: 10.1016/j.neuroscience.2007.09.027. Epub 2007 Sep 20. PMID: 18329813.

Chemical Properties

Cas No. 479347-86-9 SDF
Chemical Name sodium 6-nitro-7-sulfamoylbenzo[f]quinoxaline-2,3-bis(olate)
Canonical SMILES O=S(N)(C1=CC=CC2=C1C([N+]([O-])=O)=CC(N=C3[O-])=C2N=C3[O-])=O.[Na+].[Na+]
Formula C12H6N4O6SNa2 M.Wt 380.24
Solubility DMF: 1 mg/ml,DMSO: 20 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6299 mL 13.1496 mL 26.2992 mL
5 mM 0.526 mL 2.6299 mL 5.2598 mL
10 mM 0.263 mL 1.315 mL 2.6299 mL
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