6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮

• 常用名: 6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮
• 英文名: Licostinel
• CAS号: 153504-81-5
• 分子量: 276.03
• 密度: 1.757g/cm3
• 沸点: N/A
• 分子式: C₈H₃Cl₂N₃O₄
• 熔点: N/A
• 闪点: N/A

6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮用途

Licostinel(ACEA-1021)是一种甘氨酸受体拮抗剂(IC50:59nM)。Licostinel具有神经保护活性[1][2][3]。

6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮名称

• 中文名: 利可替奈
• 英文名: 6,7-dichloro-5-nitro-1,4-dihydroquinoxaline-2,3-dione

6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮生物活性

• 描述: Licostinel(ACEA-1021)是一种甘氨酸受体拮抗剂(IC50:59nM)。Licostinel具有神经保护活性[1][2][3]。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 靶点实验:

  59 nM (glycine receptor)[1]

• 体内研究: 动物模型：fisher344大鼠和CD-1小鼠大脑中动脉闭塞的永久性模型。Wistar和Sprague-Dawley大鼠局灶性缺血的瞬态模型[2剂量：5 mg/kg推注3.5 mg/kg/h持续6小时,10 mg/kg推注7.0 mg/kg/h持续6h给药：单次静脉注射推注持续输注结果：梗死面积减小。动物模型：雄性Sprague-Dawley大白鼠[3]剂量：20、40、80 mg/kg腹膜内注射(i.p.)推注7 mg/kg/h,30分钟给药：静脉注射(i.v.)持续输注结果：以剂量依赖的方式降低大鼠大脑中抑郁和脑电图活动的传播率。
• 参考文献:

  [1]. Zhou ZL, et al. Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists. Bioorg Med Chem. 2003 Apr 17;11(8):1769-80.

  [2]. Albers GW, et al. Dose escalation study of the NMDA glycine-site antagonist licostinel in acute ischemic stroke. Stroke. 1999 Mar;30(3):508-13.

  [3]. Martin H, et al. Effects of glycine receptor antagonism on spreading depression in the rat. Neurosci Lett. 1994 Oct 24;180(2):285-9.

6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮物理化学性质

• 密度: 1.757g/cm3
• 分子式: C₈H₃Cl₂N₃O₄
• 分子量: 276.03
• 精确质量: 274.95000
• PSA: 111.54000
• LogP: 1.95460
• InChIKey: CHFSOFHQIZKQCR-UHFFFAOYSA-N
• SMILES: O=c1[nH]c2cc(Cl)c(Cl)c([N+](=O)[O-])c2[nH]c1=O
• 折射率: 1.647
• 储存条件: 2-8°C， 密封， 干燥

6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮靶点实验

查看更多实验

实验名称：Binding affinity towards rat brain NMDA receptor glycine site expressed in Xenopus oo... 来源：ChEMBL 靶标：Glutamate receptor ionotropic, NMDA 1 External Id：CHEMBL748763

实验名称：Potency for the N-methyl-D-aspartate glutamate receptor 1 glycine site by displacemen... 来源：ChEMBL 靶标：Glutamate receptor ionotropic, NMDA 1 External Id：CHEMBL752487

实验名称：Reduction of infarct volume in rat with distal middle cerebral artery occlusion at to... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL824799

实验名称：Binding affinity at glycine binding site of NMDA receptor in rat cortical membranes b... 来源：ChEMBL 靶标：Glutamate receptor ionotropic, NMDA 3A External Id：CHEMBL748105

实验名称：In vivo effective dose of compound to protect mice from quinolinic acid seizures upon... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL834101

实验名称：Reduction of infarct volume in rat with proximal middle cerebral artery occlusion at ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL825595

实验名称：In vivo effective dose to protect the mouse (DBA/2J) from audiogenic seizures upon in... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL834191

实验名称：Ability to prevent NMDA-induced hyperlocomotion in the mouse following iv administrat... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL741313

实验名称：Displacement of [3H]-AMPA from Ionotropic glutamate receptor AMPA of rat cortical mem... 来源：ChEMBL 靶标：Glutamate receptor 1 External Id：CHEMBL698739

实验名称：ASTRAZENECA: Octan-1-ol/water (pH7.4) distribution coefficent measured by a shake fl... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3301363

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6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮英文别名

• 6,7-Dichloro-5-nitro-2,3-quinoxalinedione
• Licostinel
• 5-Nitro-6,7-dichloro-2,3-quinoxalinedione
• 2,3-Quinoxalinedione,6,7-dichloro-1,4-dihydro-5-nitro
• 5-nitro-6,7-dichloro-1,4-dihydroquinoxaline-2,3-dione
• ACEA-1021
• 6,7-dichloro-1,4-dihydro-8-nitro-2,3-quinoxalinedione
• 1,4-dihydro-6,7-dichloro-5-nitroquinoxalin-2,3-dione
• 6,7-Dichloro-1,4-dihydro-5-nitro-2,3-quinoxalinedione