607742-69-8

• 常用中文名：英特匹定
• 常用英文名：SB742457
• CAS号：607742-69-8
• 分子式：C₁₉H₁₉N₃O₂S
• 分子量：353.438
• 相关类别： 生物化工 抑制剂 神经信号通路(Neuronal Signaling) 5-HT Receptor 拮抗剂
• 发布时间：2018-08-03 18:29:20
• 更新时间：2024-01-02 20:51:05
• SB742457是5-HT6受体拮抗剂,pKi为9.63,比对其它受体的抑制性高100倍以上。

名称

• 中文名: 3-苯磺酰基-8-(哌嗪-1-基)喹啉
• 英文名: 3-(benzenesulfonyl)-8-piperazin-1-ylquinoline
• 中文别名: 英特匹定; 渥曼青霉素; 3-苯基磺酰基-8-(哌嗪-1-基)喹啉
• 英文别名: SB-742,457; Quinoline,3-(phenylsulfonyl)-8-(1-piperazinyl); RVT-101; GSK-742457; 3-(phenylsulfonyl)-8-(piperazin-1-yl)quinoline; Intepirdine; Quinoline, 3-(phenylsulfonyl)-8-(1-piperazinyl)-; UNII-2IOB2M82HY; SB-742457; 3-(Phenylsulfonyl)-8-(1-piperazinyl)quinoline; SB742457

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 608.3±45.0 °C at 760 mmHg
• 分子式: C₁₉H₁₉N₃O₂S
• 分子量: 353.438
• 闪点: 321.7±28.7 °C
• 精确质量: 353.119812
• PSA: 70.68000
• LogP: 2.10
• 外观性状: 白色至类白色粉末
• 蒸汽压: 0.0±1.7 mmHg at 25°C
• 折射率: 1.649
• 储存条件: -20℃

生物活性

• 描述: SB742457是5-HT6受体拮抗剂,pKi为9.63,比对其它受体的抑制性高100倍以上。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Callaghan CK, Hok V, Della-Chiesa A, et al. Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457. Neuropharmacology. 2012 Oct;63(5):890-7.

  [2]. Codony X, Vela JM, Ramírez MJ. 5-HT(6) receptor and cognition. Curr Opin Pharmacol. 2011 Feb;11(1):94-100.

  [3]. Maher-Edwards G, Dixon R, Hunter J, et al. SB-742457 and donepezil in Alzheimer disease: a randomized, placebo-controlled study. Int J Geriatr Psychiatry. 2011 May;26(5):536-44.

  [4]. Maher-Edwards G, Zvartau-Hind M, Hunter AJ, et al. Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Alzheimer's disease. Curr Alzheimer Res. 2010 Aug;7(5):374-85.

  [5]. Upton N, Chuang TT, Hunter AJ, Virley DJ. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics. 2008 Jul;5(3):458-69.

  [6]. SB-742457

合成路线

110-85-0 607743-09-9 ~73% 607742-69-8

文献：GLAXO GROUP LIMITED Patent: WO2005/26125 A1, 2005 ; Location in patent: Page/Page column 21-22 ; WO 2005/026125 A1

110-85-0 866782-60-7 ~84% 607742-69-8

文献：GLAXO GROUP LIMITED Patent: WO2007/39238 A1, 2007 ; Location in patent: Page/Page column 14-16 ;

110-85-0 1429304-29-9 ~69% 607742-69-8

文献：Emmett, Edward J.; Hayter, Barry R.; Willis, Michael C. Angewandte Chemie - International Edition, 2013 , vol. 52, # 48 p. 12679 - 12683 Angew. Chem., 2013 , vol. 125, # 48 p. 12911 - 12915,5

847727-21-3 ~% 607742-69-8

文献：Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890

1429304-29-9 ~% 607742-69-8

文献：Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890

611-33-6 ~% 607742-69-8

文献：Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890

607743-10-2 ~% 607742-69-8

文献：Journal of Medicinal Chemistry, , vol. 57, # 9 p. 3884 - 3890