Flunarizine-d₈ dihydrochloride  (Synonyms: 盐酸氟桂利嗪-d₈)

Flunarizine-d₈ dihydrochloride is deuterated labeled Flunarizine dihydrochloride (HY-B0358A). Flunarizine dihydrochloride is a potent dual Na⁺/Ca²⁺ channel (T-type) blocker. Flunarizine dihydrochloride is a D₂ dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects^{[1][2][3][4][5]}.

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。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Flunarizine dihydrochloride 阻断钠电流 (I_Na) 和钙电流 (I_Ca)，IC₅₀ 在培养的大鼠皮层中的值分别为 0.94 μM 和 1.77 μM分别对神经元^[3]。
Flunarizine dihydrochloride (10 和 30 μM；24 小时) 对嗜铬细胞有细胞毒性作用^[5]。
Flunarizine dihydrochloride (1-30 μM) 在浓度为 3-10 μM 时对嗜铬细胞产生明显的细胞保护作用^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Flunarizine dihydrochloride (腹膜内注射；30 mg/kg；一次) 保护小鼠免受脂多糖 (LPS) 诱导的急性肺损伤 (ALI)^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

485.47

C₂₆H₂₀D₈Cl₂F₂N₂

30484-77-6

盐酸氟桂利嗪-d₈

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

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

  [2]. Hong-Seob So, et al. Protective effect of T-type calcium channel blocker flunarizine on cisplatin-induced death of auditory cells. Hear Res. 2005 Jun;204(1-2):127-39.  [Content Brief]

  [3]. Novalbos J, et al. Effects of dotarizine and flunarizine on chromaffin cell viability and cytosolic Ca2+. Eur J Pharmacol. 1999 Feb 5;366(2-3):309-17.  [Content Brief]

  [4]. Qing Ye, et al. Flunarizine blocks voltage-gated Na(+) and Ca(2+) currents in cultured rat cortical neurons: A possible locus of action in the prevention of migraine. Neurosci Lett. 2011 Jan 10;487(3):394-9.  [Content Brief]

  [5]. Wan L, et al. Mibefradil and Flunarizine, Two T-Type Calcium Channel Inhibitors, Protect Mice against Lipopolysaccharide-Induced Acute Lung Injury. Mediators Inflamm. 2020 Nov 10;2020:3691701.  [Content Brief]

  [6]. Celia M Santi, et al. Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403.  [Content Brief]