Dronedarone

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Chemical Structure| 141626-36-0 同义名 : SR 33589
CAS号 : 141626-36-0
货号 : A404830
分子式 : C31H44N2O5S
纯度 : 99%
分子量 : 556.756
MDL号 : MFCD00910331
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(89.81 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

动物实验配方:
生物活性
描述 Dronedarone is an amiodarone-like benzofuran which lacks the iodine moiety and presents a methane sulfonyl group that decreases its lipophilicity, thus shortening the half-life and decreasing tissue accumulation. Dronedarone blocks multiple cardiac ion channels and β-adrenoceptors, presenting electrophysiological characteristics of all four Vaughan-Williams classes of antiarrhythmic drugs. Dronedarone was more effective than placebo in maintaining sinus rhythm in patients with paroxysmal and/or persistent AF and was also effective for ventricular rate control during AF (Atrial fibrillation) recurrences, providing incremental rate control on top of standard drugs in permanent AF[3]. Dronedarone decreases the incidence of AF recurrence and the ventricular rate during recurrence. Dronedarone increases mortality in patients with permanent AF and those with moderate-severe heart failure, and should thus be avoided in these populations. Dronedarone is less effective than amiodarone but also has less toxicity[4]. Furthermore, the beneficial effects of oral dronedarone on ventricular rate control were maintained during exercise and sustained with continued therapy. Oral dronedarone was generally well tolerated in the treatment of adult patients with AF and/or atrial flutter in clinical studies[5].
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
NCT01288352 Atrial Fibrillation ... 展开 >> Stroke 收起 << Phase 4 Active, not recruiting November 2019 Belgium ... 展开 >> 14 Sites Different, Belgium Czech Republic 4 Sites Different, Czech Republic Denmark 2 Sites Different, Denmark France 2 Sites Different, France Germany 51 Sites Different, Germany Italy 12 Sites Different, Italy Netherlands 13 Sites Different, Netherlands Poland 5 Sites Different, Poland Spain 10 Sites Different, Spain Switzerland 5 Sites Different, Switzerland United Kingdom 22 Sites Different, United Kingdom 收起 <<
NCT03607123 - Active, not recruiting July 4, 2022 China, Jiangsu ... 展开 >> The First Affiliated Hospital of Nanjing Medical University Nanjing, Jiangsu, China, 201129 收起 <<
NCT00911508 Atrial Fibrillation ... 展开 >> Arrhythmia 收起 << Not Applicable Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

8.98mL

1.80mL

0.90mL

17.96mL

3.59mL

1.80mL

参考文献

[1]Piccinni C, Raschi E, et al. Trends in antiarrhythmic drug use after marketing authorization of dronedarone: comparison between Emilia Romagna (Italy) and Sweden. Eur J Clin Pharmacol. 2013 Mar;69(3):715-20.

[2]Benaim G, Paniz Mondolfi AE. The emerging role of amiodarone and dronedarone in Chagas disease. Nat Rev Cardiol. 2012 Oct;9(10):605-9.

[3]Tamargo J, López-Farré A, Caballero R, Delpón E. Dronedarone. Drugs Today (Barc). 2011;47(2):109-133

[4]Tadros R, Nattel S, Andrade JG. Dronedarone: Basic Pharmacology and Clinical Use. Card Electrophysiol Clin. 2016;8(2):453-465

[5]Hoy SM, Keam SJ. Dronedarone. Drugs. 2009;69(12):1647-1663