794466-70-9

• 常用中文名：维那卡兰
• 常用英文名：Vernakalant
• CAS号：794466-70-9
• 分子式：C₂₀H₃₁NO₄
• 分子量：349.464
• 相关类别： 信号通路 跨膜转运 钾通道
• 发布时间：2018-03-15 08:00:00
• 更新时间：2024-01-02 23:19:00
• Vernakalant(RSD-1235)是混合型离子通道阻断剂,在2到5 mg/kg剂量下,能终止急性心房颤动。

名称

• 中文名: 维那卡兰
• 英文名: (3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]pyrrolidin-3-ol
• 英文别名: (3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]-3-pyrrolidinol; (1R,2R)-2-[(3R)-hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)cyclohexane; Kynapid; Vernakalant; 3-Pyrrolidinol, 1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]-, (3R)-; Brinavess; (1R-{2R-[2-(3,4-dimethoxyphenyl)-ethoxy]-cyclohex-2-yl})-pyrrolidin-3R-ol; (3R)-1-{(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl}pyrrolidin-3-ol; RSD 1235; (3R)-1-{(1R,2R)-2-[2-(3,4-Dimethoxyphenyl)ethoxy]cyclohexyl}-3-pyrrolidinol; 1R-(2R-(2-(3,4-dimethoxy-phenyl)-ethoxy)-cyclohexyl)-pyrrolidin-3R-ol; Vernakalant [INN:BAN]; UNII-9G468C8B13; cc-484; Vernakalant [INN]; (3R)-1-{(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl}pyrrolidinol

物化性质

• 密度: 1.1±0.1 g/cm3
• 沸点: 479.0±45.0 °C at 760 mmHg
• 分子式: C₂₀H₃₁NO₄
• 分子量: 349.464
• 闪点: 243.5±28.7 °C
• 精确质量: 349.225311
• PSA: 51.16000
• LogP: 2.40
• 蒸汽压: 0.0±1.3 mmHg at 25°C
• 折射率: 1.557
• 储存条件: 室温，干燥

生物活性

• 描述: Vernakalant(RSD-1235)是混合型离子通道阻断剂,在2到5 mg/kg剂量下,能终止急性心房颤动。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钾通道
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Dorian, Paul MD et al. The Effect of Vernakalant (RSD1235), an Investigational Antiarrhythmic Agent, on Atrial Electrophysiology in Humans. Journal of Cardiovascular Pharmacology:July 2007 - Volume 50 -Issue 1 - pp 35-40.

  [2]. Jodene Eldstrom et al. The Molecular Basis of High-Affinity Binding of the Antiarrhythmic Compound Vernakalant (RSD1235) to Kv1.5 Channels. Molecular Pharmacology December 2007 vol. 72 no. 6 1522-1534

  [3]. Vernakalant. Too dangerous in atrial fibrillation.Prescrire Int. 2012 May;21(127):119-22.

  [4]. Blomstr?m-Lundqvist C, Blomstr?m P.Safety and efficacy of pharmacological cardioversion of atrial fibrillation using intravenous vernakalant, a new antiarrhythmic drug with atrial selectivity.Expert Opin Drug Saf. 2012 Jul;11(4):671-9. Epub 2012 May 26.

  [5]. Bash LD, Buono JL, Davies GM, Martin A, Fahrbach K, Phatak H, Avetisyan R, Mwamburi M.Systematic review and meta-analysis of the efficacy of cardioversion by vernakalant and comparators in patients with atrial fibrillation.Cardiovasc Drugs Ther. 2012 Apr;

合成路线

906802-36-6 ~77% 794466-70-9

文献：CARDIOME PHARMA CORP. Patent: WO2006/88525 A1, 2006 ; Location in patent: Page/Page column 118; 127-128 ;

1370354-69-0 ~% 794466-70-9

文献：ALPHORA RESEARCH INC.; GORIN, Boris; DIXON, Craig Edward; OUDENES, Jan; BEJAN, Elena Valentina; KINSMAN, Aaron Cleveland Patent: WO2012/40846 A1, 2012 ; Location in patent: Page/Page column 22-23 ;

795281-92-4 ~% 794466-70-9

文献：ASTELLAS PHARMA INC. Patent: WO2006/75778 A1, 2006 ; Location in patent: Page/Page column 26-28 ;

7417-21-2 ~% 794466-70-9

文献：Limanto, John; Ashley, Eric R.; Yin, Jingjun; Beutner, Gregory L.; Grau, Brendan T.; Kassim, Amude M.; Kim, Mary M.; Klapars, Artis; Liu, Zhijian; Strotman, Hallena R.; Truppo, Matthew D. Organic Letters, 2014 , vol. 16, # 10 p. 2716 - 2719

822-87-7 ~% 794466-70-9

文献：Limanto, John; Ashley, Eric R.; Yin, Jingjun; Beutner, Gregory L.; Grau, Brendan T.; Kassim, Amude M.; Kim, Mary M.; Klapars, Artis; Liu, Zhijian; Strotman, Hallena R.; Truppo, Matthew D. Organic Letters, 2014 , vol. 16, # 10 p. 2716 - 2719

1360617-31-7 ~% 794466-70-9

文献：Limanto, John; Ashley, Eric R.; Yin, Jingjun; Beutner, Gregory L.; Grau, Brendan T.; Kassim, Amude M.; Kim, Mary M.; Klapars, Artis; Liu, Zhijian; Strotman, Hallena R.; Truppo, Matthew D. Organic Letters, 2014 , vol. 16, # 10 p. 2716 - 2719

795282-03-0 ~% 794466-70-9

文献：CARDIOME PHARMA CORP.; ROTH, Carol, J. Patent: WO2006/138673 A2, 2006 ; Location in patent: Page/Page column 49; 74-75 ;

1370354-67-8 ~% 794466-70-9

文献：ALPHORA RESEARCH INC.; GORIN, Boris; DIXON, Craig Edward; OUDENES, Jan; BEJAN, Elena Valentina; KINSMAN, Aaron Cleveland Patent: WO2012/40846 A1, 2012 ; Location in patent: Page/Page column 19 ;

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