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Flunarizine 2HCl

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Chemical Structure| 30484-77-6 同义名 : Flunarizine (hydrochloride);KW-3149;EINECS 250-216-6;Flunarizine HCl;Flunarizine hydrochloride;R14950;Flunarizine dihydrochloride
CAS号 : 30484-77-6
货号 : A165907
分子式 : C26H28Cl2F2N2
纯度 : 95%
分子量 : 477.417
MDL号 : MFCD00058198
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(104.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.09 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Calcium Channel

    Calcium channel, Ki:68 nM
描述 Flunarizine dihydrochloride (FHC), a calcium antagonist, is used for the prophylaxis to migraine. The solubility of the poorly soluble FHC was successfully improved by preparing it as a nano emulsion[3]. The most common indication for flunarizine use was chronic migraine, followed by migraine with aura, sporadic hemiplegic migraine, familial hemiplegic migraine and new daily persistent headache with migrainous features. The most common dose used was 10 mg per day. The most common adverse events were tiredness, mood change and weight gain[4]. Moreover, benefit of flunarizine prophylaxis on headache severity, frequency, and duration in children with Sturge-Weber syndrome without severe side effects[5]. In an 8-week study, 10 mg/d flunarizine is more effective than 50 mg/d topiramate for CM (Chronic migraine) prophylaxis in patients[6]. Adding tSNS (transcutaneous supraorbital neurostimulation) to flunarizine can improve the therapeutic efficacy of migraine prophylaxis without increasing the adverse effects[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03461874 Migraine Without Aura Not Applicable Recruiting July 15, 2021 Italy ... 展开 >> Fondazione IRCCS Istituto Neurologico C. Besta, Neuroalgology Unit Recruiting Milano, Italy, 20133 Contact: Licia Grazzi, MD       licia.grazzi@istituto-besta.it    Principal Investigator: Licia Grazzi, MD 收起 <<
NCT02580968 Migraine Not Applicable Completed - China ... 展开 >> Longhua Hospital,Shanghai University of Traditional Chinese Medicine Shanghai, China, 200032 收起 <<
NCT02747940 Chronic Pain ... 展开 >>Chronic Migraine Fibromyalgia 收起 << Phase 4 Recruiting - Taiwan ... 展开 >> Headache Center, Teipei Veterans General Hospital Recruiting Taipei, Taiwan, 112 Contact: Shuu-Jiun Wang, MD    +886-2-28712121 ext 2425    sjwang@vghtpe.gov.tw    Contact: Jong-Ling Fuh, MD    +886-2-28712121 ext 3256    jlfuh@vghtpe.gov.tw    Principal Investigator: Shuu-Jiun Wang, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.95mL

4.19mL

2.09mL
参考文献

[1]Kotake H, Kinugawa T, et al.Actions of flunarizine dihydrochloride on the electrical activity of isolated guinea-pig papillary muscle and rabbit sino-atrial node. Res Commun Chem Pathol Pharmacol. 1988 Nov;62(2):147-60.

[2]Fagbemi O, Kane KA, et al. The effects of verapamil, prenylamine, flunarizine and cinnarizine on coronary artery occlusion-induced arrhythmias in anaesthetized rats. Br J Pharmacol. 1984 Sep;83(1):299-304.

[3]Newton MJ, Harjot K. Fabrication, Characterization, In vitro Evaluation of Solid Lipid Nanoemulsion of Flunarizine dihydrochloride for Nasal Delivery. Antiinflamm Antiallergy Agents Med Chem. 2017; 15(3):204‐220

[4]Karsan N, Palethorpe D, Rattanawong W, Marin JC, Bhola R, Goadsby PJ. Flunarizine in migraine-related headache prevention: results from 200 patients treated in the UK. Eur J Neurol. 2018; 25(6):811‐817

[5]Gallop F, Fosi T, Prabhakar P, Aylett SE. Flunarizine for Headache Prophylaxis in Children With Sturge-Weber Syndrome. Pediatr Neurol. 2019; 93:27‐33

[6]Lai KL, Niddam DM, Fuh JL, et al. Flunarizine versus topiramate for chronic migraine prophylaxis: a randomized trial. Acta Neurol Scand. 2017;135(4):476‐483

[7]Jiang L, Yuan DL, Li M, et al. Combination of flunarizine and transcutaneous supraorbital neurostimulation improves migraine prophylaxis. Acta Neurol Scand. 2019;139(3):276‐283