NBQX |
| Catalog No.GC14156 |
NBQX is a highly selective and competitive AMPA receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118876-58-7
Sample solution is provided at 25 µL, 10mM.
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NBQX is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity,besides,It has antiepileptic effects. NBQX has little or no affinity for glutamate recognition sites on the NMDA receptor complex[1-3].
NBQX is highly selective. The IC50 value for inhibition of AMPA-evoked inward currents is 0.4 µM for NBQX. While NBQX inhibits NMDA-induced currents with IC50 value of 60 µM[4]. NBQX prevents kainic acid (KA)-induced cell death in cultures of rat cerebellar granule cells (CGCs) [5].
NBQX(5mg/kg; 8days;i.p) attenuate alcohol-withdrawal induced depression in male rats and NBQX (5 and 10 mg/kg) significantly attenuated percent alcohol intake[6-7]. NBQX(20 mg/kg, i.p.;3days) increased PNNs (WFA), tenascin-R, aggrecan and Neurocan in the medial prefrontal cortex in pentylenetetrazole(PTZ)-treated rats[8].Although NBQX had previously been shown to be an effective anticonvulsant, it had the opposite effect in TMeV-induced seizure models. Treatment with NBQX(22.5 mg/kg ;i.p;twice daily) significantly increased the number of mice with seizures and significantly increased mortality in the mice[9].
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]. Lippman-Bell JJ, Rakhade SN, et,al.AMPA receptor antagonist NBQX attenuates later-life epileptic seizures and autistic-like social deficits following neonatal seizures. Epilepsia. 2013 Nov;54(11):1922-32. doi: 10.1111/epi.12378. Epub 2013 Oct 1. PMID: 24117347; PMCID: PMC4262152.
[3]. Potschka H, LÖscher W, et,al.LU 73068, a new non-NMDA and glycine/NMDA receptor antagonist: pharmacological characterization and comparison with NBQX and L-701,324 in the kindling model of epilepsy. Br J Pharmacol. 1998 Nov;125(6):1258-66. doi: 10.1038/sj.bjp.0702172. PMID: 9863655; PMCID: PMC1565685.
[4]. Mathiesen C, Varming T, et,al. In vivo and in vitro evaluation of AMPA receptor antagonists in rat hippocampal neurones and cultured mouse cortical neurones. Eur J Pharmacol. 1998 Jul 24;353(2-3):159-67. doi: 10.1016/s0014-2999(98)00401-4. PMID: 9726646.
[5]. Verdaguer E, GarcÍa-JordÀ E, et,al.Kainic acid-induced neuronal cell death in cerebellar granule cells is not prevented by caspase inhibitors. Br J Pharmacol. 2002 Mar;135(5):1297-307. doi: 10.1038/sj.bjp.0704581. PMID: 11877339; PMCID: PMC1573245.
[6]. Getachew B, Tizabi Y. Both Ketamine and NBQX Attenuate Alcohol-Withdrawal Induced Depression in Male Rats. J Drug Alcohol Res. 2019;8:236069. doi: 10.4303/jdar/236069. PMID: 31032138; PMCID: PMC6483102.
[7]. Ruda-Kucerova J, 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.
[8]. 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.
[9]. 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.
| Cell experiment [1]: | |
|
Cell lines |
Mouse neocortical neurones |
|
Preparation Method |
Cells are continuously superfused with extracellular saline at a rate of 2.5 ml/min. After giga-seal formation the whole cell configuration is obtained by suction.The holding potential is - 60 mV and at the start of each experiment the current is measured continuously for 30 s to ensure a stable baseline. Agonist-containing solutions are delivered to the chamber through a custom-made gravity-driven flowpipe, the tip of which is placed approximately 50 µm from the cell. Application is triggered when the tubing connected to the flowpipe is compressed by a valve controlled by the Pulse software. In general, agonists are applied for 1.5 or 3 s every 45 s. The sample interval during application is 600 µs. After stable responses are obtained, the extracellular saline as well as the agonist-containing solution are replaced by solutions containing NBQX to be tested. NBQX is present until responses of a repeatable amplitude are achieved. Currents are measured at the plateau phase of the responses just before deactivation. |
|
Reaction Conditions |
0.1 µM - 100 µM |
|
Applications |
NBQX is highly selective. The IC50 value for inhibition of AMPA-evoked inward currents is 0.4 µM for NBQX. While NBQX inhibits NMDA (N-methyl-d-aspartic acid) -induced currents with IC50 value of 60 µM. |
| Animal experiment [2]: | |
|
Animal models |
Male Wistar rats |
|
Preparation Method |
Rat were exposed to EtOH vapor daily for 4 h such that an average of BAC of 160 mg% was achieved daily. then treated daily with NBQX (5 mg/kg) and evaluated for their behavior approximately 18 h later. |
|
Dosage form |
5mg/kg;8days;i.p |
|
Applications |
NBQX Attenuate Alcohol-Withdrawal Induced Depression in Male Rats. |
|
References: [1]. Mathiesen C, Varming T, et,al. In vivo and in vitro evaluation of AMPA receptor antagonists in rat hippocampal neurones and cultured mouse cortical neurones. Eur J Pharmacol. 1998 Jul 24;353(2-3):159-67. doi: 10.1016/s0014-2999(98)00401-4. PMID: 9726646. |
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| Cas No. | 118876-58-7 | SDF | |
| Chemical Name | 6-nitro-2,3-dioxo-1,2,3,4-tetrahydrobenzo[f]quinoxaline-7-sulfonamide | ||
| Canonical SMILES | O=S(N)(C1=CC=CC(C1=C2[N+]([O-])=O)=C(C(NC3=O)=C2)NC3=O)=O | ||
| Formula | C12H8N4O6S | M.Wt | 336.28 |
| Solubility | DMSO : ≥ 75 mg/mL (223.03 mM); 1 M NaOH : 1 mg/mL (2.97 mM; ultrasonic and warming and heat to 60°C); H2O : < 0.1 mg/mL (insoluble) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9737 mL | 14.8686 mL | 29.7371 mL |
| 5 mM | 0.5947 mL | 2.9737 mL | 5.9474 mL |
| 10 mM | 0.2974 mL | 1.4869 mL | 2.9737 mL |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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