英特匹定

• 常用名: 英特匹定
• 英文名: SB742457
• CAS号: 607742-69-8
• 分子量: 353.438
• 密度: 1.3±0.1 g/cm3
• 沸点: 608.3±45.0 °C at 760 mmHg
• 分子式: C₁₉H₁₉N₃O₂S
• 熔点: N/A
• 闪点: 321.7±28.7 °C

英特匹定用途

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。

英特匹定名称

• 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

英特匹定生物活性

• 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

英特匹定物理化学性质

• 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
• InChIKey: JJZFWROHYSMCMU-UHFFFAOYSA-N
• SMILES: O=S(=O)(c1ccccc1)c1cnc2c(N3CCNCC3)cccc2c1
• 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℃

英特匹定靶点实验

查看更多实验

实验名称：Antialzheimer activity against oligomeric amyloid beta (25 to 35) induced Sprague-Daw... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL5373264

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Displacement of [3H]-LSD from human 5HT-6 receptor expressed in HEK293 cell membranes... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 6 External Id：CHEMBL5373265

实验名称：Antagonist activity at recombinant human Ga16-coupled 5HT2A receptor expressed in CHO... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2A External Id：CHEMBL4685409

实验名称：Thermal Shift Assay. Domain: start/stop: N44-E168 来源：ChEMBL 靶标：Bromodomain-containing protein 4 External Id：CHEMBL5061518

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu... 来源：NCGC External Id：CYP2C9536

实验名称：Incucyte cell viability with HEK293T 来源：ChEMBL 靶标：HEK-293T External Id：CHEMBL5058565

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英特匹定英文别名

• SB-742,457
• Quinoline,3-(phenylsulfonyl)-8-(1-piperazinyl)
• RVT-101
• GSK-742457
• 3-(phenylsulfonyl)-8-(piperazin-1-yl)quinoline
• Intepirdine
• UNII-2IOB2M82HY
• SB-742457
• 3-(Phenylsulfonyl)-8-(1-piperazinyl)quinoline
• SB742457