Bioactivity | 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]. |
Invitro | 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 (INa) 和钙电流 (ICa),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. 0 --> Flunarizine-d8 dihydrochloride 相关抗体: |
In Vivo | 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. |
Formula | C26H20D8Cl2F2N2 |
Molar Mass | 485.47 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [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. [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. [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. [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. [6]. Celia M Santi, et al. Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. |