97730-95-5

• 常用中文名：(±)-SDZ-201 106
• 常用英文名：DPI 201-106
• CAS号：97730-95-5
• 分子式：C₂₉H₃₀N₄O₂
• 分子量：466.57400
• 相关类别： 信号通路 跨膜转运 钠通道
• 发布时间：2016-04-24 19:20:10
• 更新时间：2024-01-08 17:58:22
• DPI 201-106(SDZ 201106)是一种强心剂,具有协同肌膜和细胞内作用机制。DPI 201-106显示了对电压门控钠通道(VGSC)的心脏选择性调节,从而产生正性肌力效应[1][2][3]。

名称

• 中文名: SDZ-201106(±),(DPI-201106)
• 英文名: 4-[3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropoxy]-1H-indole-2-carbonitrile
• 英文别名: Dpi 201-106

物化性质

• 密度: 1.29g/cm3
• 沸点: 702.6ºC at 760mmHg
• 分子式: C₂₉H₃₀N₄O₂
• 分子量: 466.57400
• 闪点: 378.7ºC
• 精确质量: 466.23700
• PSA: 75.52000
• LogP: 4.06228
• 折射率: 1.692
• 储存条件: -20°C，密闭，干燥

生物活性

• 描述: DPI 201-106(SDZ 201106)是一种强心剂,具有协同肌膜和细胞内作用机制。DPI 201-106显示了对电压门控钠通道(VGSC)的心脏选择性调节,从而产生正性肌力效应[1][2][3]。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  研究领域 >> 心血管疾病
• 靶点:

  Sodium Channel[3]

• 体外研究: DPI 201-106增加了猪隔缘小梁皮肤纤维的Ca2+敏感性,EC50为0.2 nM[2]。DPI 201-106在豚鼠和大鼠左心房、小猫、兔和豚鼠乳头肌以及0.1至3μM之间的兔Langendorff灌注心脏中产生浓度依赖性正性肌力效应[2]。
• 体内研究: 在麻醉狗中,DPI 201-106 0.2 mg/kg静脉注射增加了左心室dP/dtmax。在地高辛预处理的麻醉猫中,DPI 201-106静脉注射的累积剂量为12.22 mg/kg[3]。
• 参考文献:

  [1]. G Scholtysik, et al. DPI 201-106, a novel cardioactive agent. Combination of cAMP-independent positive inotropic, negative chronotropic, action potential prolonging and coronary dilatory properties. Naunyn Schmiedebergs Arch Pharmacol.1985 May;329(3):316-25.

  [2]. G Scholtysik, et al. Interaction of DPI 201-106 with cardiac glycosides. J Cardiovasc Pharmacol. 1989 Feb;13(2):342-7.

  [3]. M Mevissen, et al. Identification of a cardiac sodium channel insensitive to synthetic modulators. J Cardiovasc Pharmacol Ther. 2001 Apr;6(2):201-12.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : NL5993340 CHEMICAL NAME : 1H-Indole-2-carbonitrile, 4-(3-(4-(diphenylmethyl)-1-piperazinyl)-2-hydroxyprop oxy-, (+-)- CAS REGISTRY NUMBER : 97730-95-5 LAST UPDATED : 199512 DATA ITEMS CITED : 4 MOLECULAR FORMULA : C29-H30-N4-O2 MOLECULAR WEIGHT : 466.63 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >3 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 40 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5600 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 47 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987