CNQX二钠盐 | 479347-85-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: CNQX二钠盐
• 英文名称: CNQX disodium salt
• 英文别名: disodium;6-cyano-7-nitroquinoxaline-2,3-diolate
• CAS: 479347-85-8
• 化学式: C9H2N4Na2O4
• 分子量: 276.12
• InChiKey: YCXDDPGRZKUGDG-UHFFFAOYSA-L

物化性质

• 溶解度：
  DMSO 中≥27.6 mg/mL；不溶于乙醇；不溶于水

计算性质

• 辛醇/水分配系数(LogP)：
  -6.44
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  142
• 氢给体数：
  0
• 氢受体数：
  7

制备方法与用途

生物活性

CNQX disodium (FG9065 disodium) 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 0.3 μM 和 1.5 μM。CNQX disodium 是一种竞争性的非 NMDA 受体拮抗剂。CNQX disodium 会阻止大鼠恐惧增强的表达。

靶点

IC50: 0.3 μM (AMPA) and 1.5 μM (kainate receptor)

体外研究

CNQX disodium (FG9065 disodium; 2-5 μM) reversibly blocks the Schaffer collateral and mossy fibre excitatory postsynaptic potential (EPSP), while sparing the fast and slow GABA-mediated inhibition in superfusion of hippocampal slices.
CNQX disodium (1-5 μM) produces a selective and dose-dependent reduction in the amplitude of the monosynaptic component of the DR-VRR recorded from lumbar spinal segments.

体内研究

CNQX disodium (FG9065 disodium; 0.75-3 mg/kg; IP; 20 min before testing) decreased the number of cocaine responses in a dose-dependent manner during the first 15-min cocaine-free interval.
The bilateral infusion of CNQX disodium (0.5 or 1.25 μg) into the amygdala or dorsal hippocampus 10 min prior to a retention test partially blocks the expression of stepdown inhibitory avoidance in rats 24 h after training. CNQX disodium causes a complete blockade at a dose of 0.5 μg.

Animal Model:	Male Wistar rats weighing 180-200 g
Dosage:	0.75, 1.5, and 3 mg/kg
Administration:	IP; 20 min before testing
Result:	Decreased the number of cocaine (IV; 0.25 mg/infusion) responses in a dose-dependent manner during the first 15-min cocaine-free interval.

文献信息

• MITIGATION OF CNS DISORDERS BY COMBINATION THERAPY USING NEUROSTEROIDS, AND AMPA BLOCKERS
  申请人：The Regents of the University of California

  公开号：US20200030304A1

  公开（公告）日：2020-01-30

  Provided are compositions and methods for treating epilepsy, including epilepsy caused by exposure to organophosphate nerve agents, that entail co-formulation and/or co-administration of a benzodiazepine, a neurosteroid and an AMPA receptor antagonist.
• [EN] MITIGATION OF CNS DISORDERS BY COMBINATION THERAPY USING NEUROSTEROIDS, AND AMPA BLOCKERS<br/>[FR] ATTÉNUATION DE TROUBLES DU SNC PAR POLYTHÉRAPIE FAISANT INTERVENIR DES NEUROSTÉROÏDES, ET DES BLOQUEURS AMPA
  申请人：UNIV CALIFORNIA

  公开号：WO2018169798A1

  公开（公告）日：2018-09-20

  Provided are compositions and methods for treating epilepsy, including epilepsy caused by exposure to organophosphate nerve agents, that entail co-formulation and/or co-administration of a benzodiazepine, a neurosteroid and an AMPA receptor antagonist.