143322-58-1

• 常用中文名：依来曲普坦
• 常用英文名：Eletriptan
• CAS号：143322-58-1
• 分子式：C₂₂H₂₆N₂O₂S
• 分子量：382.519
• 相关类别： 原料药 解热镇痛药 镇痛药
• 发布时间：2018-02-23 08:00:00
• 更新时间：2026-07-04 12:37:58
• Eletriptan(UK-116044)是一种具有高度选择性和口服活性的5-HT1B和5-HT1D受体激动剂,pKi值分别为8.0和8.9。Eletriptan对大鼠神经源性炎症标志物具有抑制作用。Eletriptan可用于研究偏头痛[1]。

名称

• 中文名: 依来曲普坦
• 英文名: eletriptan
• 中文别名: 埃立曲坦杂质; 埃立曲坦; 依来曲普坦 (ELETRIPTAN)/143-1; 来曲普坦; 氢溴酸依利曲坦; 依来曲普坦 (ELETRIPTAN); 13C,2H3]-依来曲坦; (R)-3-苄基-5-(1-(2-(吡咯烷-1-基)乙基)-1H-吲哚-3-基)-1,2,4-恶二唑; 依利曲坦; 依立曲坦-D3; 3-[(1-甲基吡咯烷-2-基)甲基]-5-(2-苯基磺酰乙基)-1H-吲哚; 依来曲普坦杂质; (R)-依立曲坦; 5-(2-苯磺酰乙基)-3-[(1-甲基吡咯烷-2-基)甲基] -1H-吲哚; 5-[2-(苯磺酰基)乙基]-3-[1-甲基吡咯烷-2(R)-基甲基]-1H-吲哚; 伊利曲坦; 3-苄基-5-(1-(2-(吡咯烷-1-基)乙基)-1H-吲哚-3-基)-1,2,4-恶二唑
• 英文别名: 3-benzyl-5-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indol-3-yl)-1,2,4-oxadiazole; 1H-Indole, 3-(((2R)-1-methyl-2-pyrrolidinyl)methyl)-5-(2-(phenylsulfonyl)ethyl)ethyl); Tianfu Chem Eletriptan; ELETRIPTAN; EletriptanHydrobromide(ForR&DOnly); 3-{[(2R)-1-Methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole; 5-[2-(benzenesulfonyl)ethyl]-3-[(1-methyl-2-pyrrolidinyl)methyl]-1H-indole; 3-[[(R)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]indolemonohydrobromide; 5-[2-(benzenesulfonyl)ethyl]-3-[(1-Methylpyrrolidin-2-yl)Methyl]-1H-indole; (R)-5-[2-(Benzenesulfonyl)ethyl]-3-[(N-methylpyrrolidin-2-yl)methyl]-1H-indole; Eletriptan Also see: R143400; 1H-Indole,3-[[(2R)-1-Methyl-2-pyrrolidinyl]Methyl]-5-[2-(phenylsulfonyl)ethyl]; Unii-22qoo9B8ki; UK-116044,Relpax,3-[[(2R)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole; Relpax; UK-116044; 3-{[(2R)-1-Methyl-2-pyrrolidinyl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole; (R)-3-[(1-Methyl-2-pyrrolidinyl)methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-Indole; MFCD00943792; 5-(2-(Benzenesulfoyl)vinyl)-3-(1-Methylpyrrolidin-2(R)-ylmethyl)-1H-Indole; Eletriptan Impurity 6; Eletriptan //BP; 3-[[(2R)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole; 5-[2-(benzenesulfonyl)ethyl]-3-{[(2R)-1-Methylpyrrolidin-2-yl]Methyl}-1H-indole; UK-116,[as hydrobromide]; Eletriptan Free Base; (R)-Eletriptan; According to triptans; 5-[2-(benzenesulfonyl)ethyl]-3-[1-methylpyrrolidin-2(R)-ylmethy] -1H-indole; 3-[(1-methylpyrrolidin-2-yl)methyl]-5-(2-phenylsulfonylethyl)-1h-indole; 5-(2-(BENZENESULFONYL)VINYL)-3-(1-METHYLPYRROLIDIN-2(R)-YLMETHYL)-1H-INDOLE; Relpax free aMine; (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole; 5-[2-(benzenesulfonyl)ethyl]-3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-1H-indole

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 613.4±55.0 °C at 760 mmHg
• 分子式: C₂₂H₂₆N₂O₂S
• 分子量: 382.519
• 闪点: 324.8±31.5 °C
• 精确质量: 382.171509
• PSA: 61.55000
• LogP: 3.08
• 外观性状: 黄色泡沫
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.634
• 储存条件: Hygroscopic, Refrigerator, Under Inert Atmosphere

生物活性

• 描述: Eletriptan(UK-116044)是一种具有高度选择性和口服活性的5-HT1B和5-HT1D受体激动剂,pKi值分别为8.0和8.9。Eletriptan对大鼠神经源性炎症标志物具有抑制作用。Eletriptan可用于研究偏头痛[1]。
• 相关类别:
  研究领域 >> 炎症/免疫
  研究领域 >> 神经疾病
  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
• 靶点:

  5-HT1B Receptor:8.0 (pKi)

  5-HT1D Receptor:8.9 (pKi)

• 体内研究: Eletriptan(10、30、100、300和1000µg/kg；静脉注射)通过选择性减少颈动脉动静脉吻合血流量和增加颈动脉血管床内的营养血流量来减少麻醉猪的总颈动脉血流量[2]。
• 参考文献:

  [1]. McCormack PL, Keating GM. Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2006;66(8):1129-49.

  [2]. Willems E, et al. Porcine carotid vascular effects of eletriptan (UK-116,044): a new 5-HT1B/1D receptor agonist with anti-migraine activity. Naunyn Schmiedebergs Arch Pharmacol. 1998 Aug;358(2):212-9.

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