NBQX disodium salt |
Katalog-Nr.GC13482 |
NBQX, ein Dinatriumsalz, wirkt als potenter, selektiver und kompetitiver Antagonist der AMPA-Rezeptoren (α-Amino-3-hydroxy-5-methyl-4-isoxazolpropionsäure).
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Cas No.: 479347-86-9
Sample solution is provided at 25 µL, 10mM.
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.
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