866455-16-5

• 常用中文名：Vernakalant-d6盐酸盐
• 常用英文名：Vernakalant-d6 hydrochloride
• CAS号：866455-16-5
• 分子式：C₂₀H₂₆D₆ClNO₄
• 分子量：391.96
• 相关类别： 信号通路 跨膜转运 钾通道
• 发布时间：2016-09-30 16:20:02
• 更新时间：2024-02-04 18:25:14
• Vernakalant-d6(盐酸盐)是氘标记的Vernakalant。

名称

• 中文名: Vernakalant-d6盐酸盐
• 英文名: 3-Pyrrolidinol, 1-[(1R,2R)-2-[2-[3,4-di(methoxy-d3)phenyl]ethoxy]cyclohexyl]-, hydrochloride, (3R)
• 英文别名: Vernakalant-d6 Hydrochloride

物化性质

• 分子式: C₂₀H₂₆D₆ClNO₄
• 分子量: 391.96
• 精确质量: 385.20200
• PSA: 51.16000
• LogP: 3.38060

生物活性

• 描述: Vernakalant-d6(盐酸盐)是氘标记的Vernakalant。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 体外研究: 氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。
• 参考文献:

  [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

  [2]. 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.

  [3]. 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

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

  [5]. 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.

  [6]. 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;26(2):167-79.