156053-89-3

• 常用中文名：爱维莫潘
• 常用英文名：Alvimopan
• CAS号：156053-89-3
• 分子式：C₂₅H₃₂N₂O₄
• 分子量：424.533
• 相关类别： 原料药 消化系统用药 胃肠动力药
• 发布时间：2018-09-22 10:50:20
• 更新时间：2026-07-01 16:17:22
• Alvimopan(LY 246736; ADL 8-2698)是新型的口服外周阿片样受体(PAM-OR)拮抗剂,IC50为1.7 nM。

名称

• 中文名: 爱维莫潘
• 英文名: Alvimopan
• 中文别名: 爱维莫潘,10 MM DMSO 溶液; 爱维莫潘相关杂质; 阿维莫泮; 爱维莫泮; 2-([(2S)-2-([(3R,4R)-4-(3-羟基苯基)-3,4-二甲基哌啶-1-基]甲基)-3-苯基丙酰]氨基)乙酸; 爱维莫潘、艾维莫潘杂质; 2-((S)-2-苄基-3-((3R,4R)-4-(3-羟苯基)-3,4-二甲基哌啶-1-基)丙酰胺O)乙酸; 阿尔维莫潘; 2-((S)-2-苄基-3-((3R,4R)-4-(3-羟基苯基)-3,4-二甲基哌啶-1-基)丙酰胺)乙酸
• 英文别名: Ly246736; N-{(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl}glycine; 2-([(2S)-2-([(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl)-3-phenylpropanoyl]amino)acetic acid; ((S)-2-benzyl-3-((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl)propanoyl)glycine; AlviMopan (ADL 8); 2-((S)-2-benzyl-3-((3R,4R)-4-(3-hydroxyphenyl)-3,4-diMethylpiperidin-1-yl)propanaMido)acetic acid; 170-1 (Dihydrate); Unii-Q153V49p3z; 2-((S)-2-Benzyl-3-((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl)propanamido)acetic a; N-[(2S)-2-[[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-diMethyl-1-piperidinyl]Methyl]-1-oxo-3-phenylpropyl]glycine; Alvimopan //BP; trans-3,4-Dimethyl-4-(3-hydroxyphenyl) piperidine; Alvimopan, 10 mM in DMSO; Evemopan; Glycine, N-((2S)-2-(((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl)methyl)-1-oxo-3-phenylpropyl); Alvimopan anhydrous; Alvimopan - Bio-X; N-{(2S)-2-Benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]propanoyl}glycine

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 684.1±55.0 °C at 760 mmHg
• 熔点: 210-213ºC
• 分子式: C₂₅H₃₂N₂O₄
• 分子量: 424.533
• 闪点: 367.5±31.5 °C
• 精确质量: 424.236206
• PSA: 89.87000
• LogP: 3.38
• 蒸汽压: 0.0±2.2 mmHg at 25°C
• 折射率: 1.572
• 储存条件: 2-8°C

生物活性

• 描述: Alvimopan(LY 246736; ADL 8-2698)是新型的口服外周阿片样受体(PAM-OR)拮抗剂,IC50为1.7 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
  信号通路 >> 神经信号通路 >> 阿片受体
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. NCBI BioAssay: 325959

  [2]. Cassel JA, et al. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol. 2005 Sep 27;520(1-3):29-36.

  [3]. Viscusi ER, et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study. Surg Endosc. 2006 Jan;20(1):64-70.

  [4]. Fukuda H, et al. The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res. 2006 Aug 2;1102(1):63-70.

  [5]. Delaney CP, et al. Phase III trial of alvimopan, a novel, peripherally acting, mu opioid antagonist, for postoperative ileus after major abdominal surgery. Dis Colon Rectum. 2005 Jun;48(6):1114-25; discussion 1125-6; author reply 1127-9.

安全

• 符号: GHS07, GHS09
• 信号词: Warning
• 危害声明: H315-H319-H400
• 警示性声明: P273-P280-P305 + P351 + P338-P337 + P313-P391
• 危险品运输编码: UN 3077 9 / PGIII
• 海关编码: 2933399090

合成路线

145603-86-7 ~% 156053-89-3

文献：Zimmerman, Dennis M.; Gidda, Jaswant S.; Cantrell, Buddy E.; Schoepp, Darryle D.; Johnson, Bryan G.; Leander, J. David Journal of Medicinal Chemistry, 1994 , vol. 37, # 15 p. 2262 - 2265

20593-63-9 ~% 156053-89-3

文献：Journal of Medicinal Chemistry, , vol. 37, # 15 p. 2262 - 2265

119193-19-0 ~% 156053-89-3

文献：Journal of Medicinal Chemistry, , vol. 37, # 15 p. 2262 - 2265

147383-72-0 ~% 156053-89-3

文献：WO2011/161646 A2, ;

1314751-83-1 ~% 156053-89-3

文献：WO2011/161646 A2, ;

上下游产品

上游产品  3
20593-63-9 119193-19-0 147383-72-0
下游产品  0

海关

海关编码	2933399090
中文概述	2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%