GlpBio

NBQX

目录号: GC14156纯度: >98.00%同义词: 二羟基喹酮,FG9202
NBQX是一种高度选择性和竞争性的AMPA受体拮抗剂。
NBQX
Cas No.: 118876-58-7
规格价格库存数量操作
1mg¥308.00现货
1
5mg¥770.00现货
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10mg¥1,190.00现货
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25mg¥2,100.00现货
1
50mg¥3,150.00现货
1
10mM (in 1mL DMSO)¥570.00现货
1
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产品描述 Description

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.

NBQX是一种高度选择性和竞争性的AMPA受体拮抗剂。NBQX具有神经保护和抗惊厥作用,并有抗癫痫作用。NBQX对NMDA受体复合体上的谷氨酸识别位点几乎没有亲和力[1-3]。

NBQX是高度选择性的。NBQX抑制AMPA诱导的内向电流的IC50值为0.4 µM。NBQX抑制NMDA诱导电流的IC50值为60 µM[4]。NBQX可预防kainic acid (KA)诱导的大鼠小脑颗粒细胞(CGCs)死亡[5]。

NBQX(5mg/kg;18h;i.p)减轻雄性大鼠酒精戒断诱导的抑郁,NBQX(5和10 mg/kg)显著降低酒精摄入量百分比[6-7]。NBQX(20 mg/kg, i.p;3days)增加戊四唑(PTZ)治疗大鼠内侧前额皮质PNNs (WFA)、tenascin-R、aggrecan和Neurocan的表达[8]。虽然NBQX先前已被证明是一种有效的抗惊厥药,但它在TMeV诱导的癫痫发作模型中具有相反的作用。NBQX治疗(22.5 mg/kg ;i.p;twice daily)显著增加了癫痫发作小鼠的数量,显著增加了小鼠的死亡率[9]。

实验参考方法 Experimental Reference Method

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.
[2].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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
118876-58-7
同义词
二羟基喹酮,FG9202
化学名
6-nitro-2,3-dioxo-1,2,3,4-tetrahydrobenzo[f]quinoxaline-7-sulfonamide
SMILES
O=S(N)(C1=CC=CC(C1=C2[N+]([O-])=O)=C(C(NC3=O)=C2)NC3=O)=O
分子式
C12H8N4O6S
分子量
336.28 g/mol
溶解性
DMSO : ≥ 75 mg/mL (223.03 mM); 1 M NaOH : 1 mg/mL (2.97 mM; ultrasonic and warming and heat to 60°C); H<sub>2</sub>O : &lt; 0.1 mg/mL (insoluble)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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