CNQX
(Synonyms: 6-氰基-7-硝基喹喔啉-2,3-二酮,FG9065) 目录号 : GC11799
CNQX是一种有效的竞争性AMPA /海藻酸酯受体(AMPA/kainate receptor)拮抗剂,IC50 分别为0.3µM和1.5µM。
Cas No.:115066-14-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
CNQX is an effective competitive antagonist of AMPA/kainate receptors, with IC50 values of 0.3µM and 1.5µM, respectively[1]. CNQX is a non-NMDA receptor antagonist[2].
In vitro, CNQX (1µM) reduces the frequency of light-induced peak potentials in retinal ganglion cells by 28%±22% and also induces voltage- and magnesium-dependent delayed spike firing[2]. CNQX (0-100 mM; 20-24 h) exhibits dose-dependent toxicity in mixed mouse cortical cells, with neuronal damage effects[3]. CNQX (20 µM) reversibly depolarizes the membrane potential of TRN neurons, inducing smaller depolarizations in thalamic relay neurons in VB[4].
In vivo, CNQX (0.5 µg; i.c.v.) can block hippocampal CA3 pyramidal cell death induced by kainic acid in ICR mice, partially attenuate the increase of p-ERK and the decrease of p-CREB, and inhibit the expression of phosphorylated ERK protein[5]. Bilateral infusion of CNQX (0.5 or 1.25µg) into the amygdala or dorsal hippocampus of rats can block the expression of startle reflex[6].
References:
[1]TAGE HONORÉ, STEVE N. DAVIES, JØRGEN DREJER, et al. Quinoxalinediones: Potent Competitive Non-NMDA Glutamate Receptor Antagonists[J]. SCIENCE.1988(241):701-703.
[2] Jeffrey S. Diamond, David R. Copenhagen. The contribution of NMDA and Non-NMDA receptors to the light-evoked input-output characteristics of retinal ganglion cells[J]. Cell Press. October, 1993:725-738.
[3]Uliasz T F , Hewett S J . A microtiter trypan blue absorbance assay for the quantitative determination of excitotoxic neuronal injury in cell culture[J]. Journal of Neuroscience Methods, 2000, 100(1-2):157-163.
[4]Sang Hun Lee,G. Govindaiah,and Charles L. Cox. Selective Excitatory Actions of DNQX and CNQX in Rat Thalamic Neurons[J].Journal of Neurophysiology, 2010(4):103.
[5]Lee J K , Choi S S , Lee H K ,et al.Effects of MK-801 and CNQX on various neurotoxic responses induced by kainic acid in mice.[J]. Molecules & Cells, 2002, 14(3):339-347.
[6]Kim M, Campeau S, Falls W A, et al. Infusion of the non-NMDA receptor antagonist CNQX into the amygdala blocks the expression of fear-potentiated startle. Behav Neural Biol, 1993, 59(1): 5-8.
CNQX是一种有效的竞争性AMPA /海藻酸酯受体(AMPA/kainate receptor)拮抗剂,IC50 分别为0.3µM和1.5µM[1]。CNQX 是一种非NMDA受体拮抗剂[2]。
在体外,CNQX(1µM)使视网膜神经节细胞的光诱发峰电位频率降低了28%±22%,还引起了电压和镁依赖性的延迟尖峰发作[2]。CNQX(0-100 mM; 20-24 h)对混合小鼠皮质细胞产生剂量依赖性的毒性,具有神经元损伤作用[3]。CNQX(20 µM)以可逆方式使TRN神经元的膜电位去极化,在VB中继神经元中诱发的去极化较小[4]。
在体内,CNQX (0.5 µg; i.c.v.)能阻断红藻氨酸诱导的ICR小鼠海马CA3区锥体细胞死亡,部分减弱p-ERK升高和p-CREB降低,抑制磷酸化ERK蛋白表达[5]。CNQX(0.5或1.25µg)双侧输注到大鼠杏仁核或背侧海马体中,可以阻断惊吓反射的表达[6]。
| Cell experiment [1]: | |
|
Cell lines |
Mixed murine cortical cell |
|
Preparation Method |
Mixed murine cortical cell cultures were exposed to kainate (0-100 mM) in the absence or presence of increasing concentrations of CNQX. Then 20-24 h later, injury was assessed by spectrophotometric measurement of lactate dehydrogenase (LDH) activity and trypan blue. |
|
Reaction Conditions |
0-100 mM; 20-24 h |
|
Applications |
There is a time-dependent increase in neuronal cell death as CNQX concentration increases. |
| Animal experiment [2]: | |
|
Animal models |
Male ICR mice |
|
Preparation Method |
CNQX were prepared in 5 % DMSO as vehicle. The i.c.v. administrations of KA, MK-801, and CNQX were performed following the procedure established by Laursen and Belknap (1986). Briefly, each mouse was injected at bregma with a 50 µl Hamilton microsyringe fitted with a 26-gauge needle that was inserted to a depth of 2.4 mm. The injection volume was 5µl. CNQX (0.5 µg) were injected 10 min prior to KA injection. |
|
Dosage form |
0.5 µg; i.c.v. |
|
Applications |
CNQX can block kainic acid-induced pyramidal cell death in the CA3 area of the mouse hippocampus, partially attenuate the increase in p-ERK and the decrease in p-CREB, and inhibit the expression of phosphorylated ERK protein. |
|
References: [1] Uliasz T F , Hewett S J . A microtiter trypan blue absorbance assay for the quantitative determination of excitotoxic neuronal injury in cell culture[J]. Journal of Neuroscience Methods, 2000, 100(1-2):157-163. |
|
| Cas No. | 115066-14-3 | SDF | |
| 别名 | 6-氰基-7-硝基喹喔啉-2,3-二酮,FG9065 | ||
| 化学名 | 7-nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-carbonitrile | ||
| Canonical SMILES | O=C1NC2=CC([N+]([O-])=O)=C(C#N)C=C2NC1=O | ||
| 分子式 | C9H4N4O4 | 分子量 | 232.16 |
| 溶解度 | ≥ 23.2mg/mL in DMSO | 储存条件 | 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℃，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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.3074 mL | 21.5369 mL | 43.0737 mL |
| 5 mM | 0.8615 mL | 4.3074 mL | 8.6147 mL |
| 10 mM | 0.4307 mL | 2.1537 mL | 4.3074 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet