153504-81-5

• 常用中文名：6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮
• 常用英文名：Licostinel
• CAS号：153504-81-5
• 分子式：C₈H₃Cl₂N₃O₄
• 分子量：276.03
• 相关类别： 研究领域 神经疾病
• 发布时间：2018-04-15 08:00:00
• 更新时间：2024-01-18 06:02:28
• 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]。

名称

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

物化性质

• 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
• 折射率: 1.647
• 储存条件: 2-8°C， 密封， 干燥

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:

  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.

合成路线

25983-13-5 ~93% 153504-81-5

文献：Keana; Kher; Sui Xiong Cai; Dinsmore; Glenn; Guastella; Huang; Ilyin; Lu; Mouser; Woodward; Weber Journal of Medicinal Chemistry, 1995 , vol. 38, # 22 p. 4367 - 4379

153505-40-9 ~88% 153504-81-5

文献：Kher, Sunil M.; Cai, Sui Xiong; Weber, Eckard; Keana, John F. W. Journal of Organic Chemistry, 1995 , vol. 60, # 18 p. 5838 - 5842

78470-95-8 ~% 153504-81-5

文献：Kher, Sunil M.; Cai, Sui Xiong; Weber, Eckard; Keana, John F. W. Journal of Organic Chemistry, 1995 , vol. 60, # 18 p. 5838 - 5842

5348-42-5 ~% 153504-81-5

文献：Keana; Kher; Sui Xiong Cai; Dinsmore; Glenn; Guastella; Huang; Ilyin; Lu; Mouser; Woodward; Weber Journal of Medicinal Chemistry, 1995 , vol. 38, # 22 p. 4367 - 4379

21641-42-9 ~% 153504-81-5

文献：Thorell, Jan-Olov; Stone-Elander, Sharon; Duelfer, Tim; Cai, Sui Xiong; Jones, Lawrence; Pfefferkorn, Heidi; Ciszewska, Grazyna Journal of Labelled Compounds and Radiopharmaceuticals, 1998 , vol. 41, # 4 p. 345 - 353

95-92-1 276238-86-9 ~% 153504-81-5

文献：Thorell, Jan-Olov; Stone-Elander, Sharon; Duelfer, Tim; Cai, Sui Xiong; Jones, Lawrence; Pfefferkorn, Heidi; Ciszewska, Grazyna Journal of Labelled Compounds and Radiopharmaceuticals, 1998 , vol. 41, # 4 p. 345 - 353

5348-42-5 95-92-1 ~% 153504-81-5

文献：Thorell, Jan-Olov; Stone-Elander, Sharon; Duelfer, Tim; Cai, Sui Xiong; Jones, Lawrence; Pfefferkorn, Heidi; Ciszewska, Grazyna Journal of Labelled Compounds and Radiopharmaceuticals, 1998 , vol. 41, # 4 p. 345 - 353

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