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CNQX disodium {[allProObj[0].p_purity_real_show]}

货号:A814876 同义名: FG9065 disodium

CNQX disodium是 AMPA/kainate 受体拮抗剂,也可作为 Kainate 受体的一部分。

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CNQX disodium 化学结构 CAS号:479347-85-8
CNQX disodium 化学结构
CAS号:479347-85-8
CNQX disodium 3D分子结构
CAS号:479347-85-8
CNQX disodium 化学结构 CAS号:479347-85-8
CNQX disodium 3D分子结构 CAS号:479347-85-8
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CNQX disodium 纯度/质量文件 产品仅供科研

货号:A814876 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AMPA receptor GluR mGluR5 NMDA receptor 其他靶点 纯度
Evans Blue 85% (Dye content)
IEM-1754 +

GluR1, IC50: 6 μM

GluR3, IC50: 6 μM

99%
Latrepirdine 2HCl 99%
(-)-Huperzine A +++

AChE (G4 form), Ki: 7 nM

98%
CTEP ++++

mGlu5, IC50: 2.2 nM

98%+
MPEP ++

mGluR5, IC50: 36 nM

99%+
Riluzole 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

CNQX disodium 生物活性

描述 CNQX disodium (FG9065 disodium), a potent and competitive AMPA/kainate receptor antagonist, displays IC50s of 0.3 μM and 1.5 μM, respectively, functioning as a competitive non-NMDA receptor antagonist[1]. CNQX disodium suppresses the expression of fear-potentiated startle in rats[5].
体内研究

CNQX disodium (FG9065 disodium; 0.75-3 mg/kg; IP; 20 min before testing) diminishes the number of cocaine responses in a dose-dependent manner during the first 15-min cocaine-free interval[4].

Bilateral infusion of CNQX disodium (0.5 or 1.25 μg) into the amygdala or dorsal hippocampus 10 min before a retention test partially impedes the expression of stepdown inhibitory avoidance in rats 24 h after training. Complete blockade is achieved with a dose of 0.5 μg[5].

体外研究

CNQX disodium (FG9065 disodium; 2-5 μM) reversibly inhibits the Schaffer collateral and mossy fiber excitatory postsynaptic potential (EPSP) while preserving fast and slow GABA-mediated inhibition in superfusion of hippocampal slices[2].

CNQX disodium (1-5 μM) induces a selective and dose-dependent decrease in the amplitude of the monosynaptic component of the DR-VRR recorded from lumbar spinal segments[3].

CNQX disodium 细胞实验

Cell Line
Concentration Treated Time Description References
noradrenergic neurons in brainstem slices 50 μM 30 min CNQX abolished gabapentin-induced pCREB activation Anesthesiology. 2008 Dec;109(6):1077-84
ARC neurons 30 μM 8 min CNQX significantly reduced the spontaneous discharge frequency of ARC neurons in inflamed rats from (2.17±0.25) Hz to (1.32±0.15) Hz (P<0.01), indicating the critical role of non-NMDA receptors in inflammation-induced neuronal activation. Acta Pharmacol Sin. 2011 Feb;32(2):160-6
Immature rat spinal cord preparations 4, 10, 25 μM 25-30 min To measure the antagonism of depolarizations induced by NMDA, kainate, or quisqualate by CNQX. In the presence of 0.75 mM Mg2+, pA2 values were 4.62 ± 0.05 (NMDA), 5.79 ± 0.01 (kainate), 5.59 ± 0.05 (quisqualate). Br J Pharmacol. 1990 Aug;100(4):850-4
Mature rat spinal cord preparations 1.0 μM To compare the depressant effects of CNQX and kynurenate on transmission from low threshold myelinated primary afferents. The EC50 for CNQX-induced depression of the monosynaptic ventral root reflex was 1.0 μM. Br J Pharmacol. 1990 Aug;100(4):850-4
rat striatal neurons 10 μM To investigate the inhibitory effect of CNQX on synaptic potentials in striatal neurons, showing that CNQX reversibly blocks the depolarizing synaptic potential evoked by stimulation of corticostriatal fibers. J Physiol. 1991 Nov;443:533-53
HEK293 cells 30 µM 5 seconds To study the inhibitory effect of CNQX on GluN1a-3A NMDAR Sci Adv. 2024 Apr 12;10(15):eadl5952

CNQX disodium 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats L5-L6 spinal nerve ligation (SNL) model Intra-LC injection 0.3 μg Single injection, behavioral testing performed 15 minutes post-injection CNQX blocked the antihypersensitivity effect of intra-LC gabapentin Anesthesiology. 2008 Dec;109(6):1077-84
Rats Water maze test Bilateral intra-LHb infusion 267 ng/side Single injection, behavioral testing performed 15 minutes post-injection To investigate the role of LHb in encoding and retrieval of spatial memory. CNQX infusion prevented encoding and retrieval but not consolidation of spatial information. Neuropsychopharmacology. 2015 Nov;40(12):2843-51
Adult Brown-Norway rats Optic nerve transection model Intravitreal injection 0.2 mM Single injection CNQX substantially reduced the nSTR and also reduced the scotopic b-wave by ~40%. J Physiol. 2004 Feb 15;555(Pt 1):153-73
Mice Awake mice Pressure injection 100 μM 10 minutes CNQX reduced the frequency and area of hotspot events, indicating that hotspot signals are generated primarily by excitatory synaptic input and stochastic voltage fluctuations within the dendrite Nat Commun. 2018 Aug 23;9(1):3388

CNQX disodium 参考文献

[1]Aqeel Imran, et al. Development, Molecular Docking, and In Silico ADME Evaluation of Selective ALR2 Inhibitors for the Treatment of Diabetic Complications via Suppression of the Polyol Pathway. ACS Omega 2022.

[2]Neuman RS, et al. Blockade of excitatory synaptic transmission by 6-cyano-7-nitroquinoxaline-2,3-dione(CNQX) in the hippocampus in vitro. Neurosci Lett. 1988 Sep 23;92(1):64-8.

[3]Alford S, et al. CNQX and DNQX block non-NMDA synaptic transmission but not NMDA-evoked locomotion in lamprey spinal cord. Brain Res. 1990 Jan 8;506(2):297-302.

[4]Pia Bäckström, et al. Attenuation of Cocaine-Seeking Behaviour by the AMPA/kainate Receptor Antagonist CNQX in Rats. Psychopharmacology (Berl). 2003 Feb;166(1):69-76.

[5]Kim M, et al. Infusion of the non-NMDA receptor antagonist CNQX into the amygdala blocks the expression of fear-potentiated startle. Behav Neural Biol. 1993 Jan;59(1):5-8.

CNQX disodium 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.62mL

0.72mL

0.36mL

18.11mL

3.62mL

1.81mL

36.22mL

7.24mL

3.62mL

CNQX disodium 技术信息

CAS号479347-85-8
分子式C9H2N4Na2O4
分子量 276.12
SMILES Code N#CC1=CC2=C([N-]C(C([N-]2)=O)=O)C=C1[N+]([O-])=O.[Na+].[Na+]
MDL No. MFCD00801053
别名 FG9065 disodium
运输蓝冰
InChI Key YCXDDPGRZKUGDG-UHFFFAOYSA-L
Pubchem ID 6093155
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 9 mg/mL(32.59 mM),配合低频超声,水浴加热至45℃,并调节pH至2,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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