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Amiodarone HCl

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Chemical Structure| 19774-82-4 同义名 : 盐酸胺碘酮 ;Amiodarone (hydrochloride);Amiodarone hydrochloride
CAS号 : 19774-82-4
货号 : A143592
分子式 : C25H30ClI2NO3
纯度 : 97%
分子量 : 681.77
MDL号 : MFCD00069204
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(29.34 mM)，配合低频超声，并水浴加热至45℃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：

2% DMSO+30% PEG 300+2% Tween 80+water 3 mg/mL

生物活性
靶点

  • Potassium Channel
描述 Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM. Amiodarone may act as an antioxidant/antiatherosclerotic agent in humans[3]. Amiodarone stimulates the accumulation of ethidium bromide by inhibiting its efflux from the cells. The effect of amiodarone is much stronger on wild-type cells compared to the mutant with inactivated ABC-transporters[4]. Chronic treatment with oral amiodarone for 4 weeks reduced Ip when myocytes were dialyzed with patch-pipettes containing either 10 mM Na+ or 80 mM Na+. Amiodarone had no effect on the voltage dependence of the pump or the affinity of the pump for extracellular K+ either after chronic treatment or during acute exposure. An amiodarone-induced inhibition of the hyperpolarizing Na(+)-K+ pump current may contribute to the action potential prolongation observed during treatment with this drug[5]. Cells treated with amiodarone were seen to have detached from the dish, with cell rounding, cytoplasmic blebbing and irregularity in shape. An increase in the sub-G1 phase fraction, from 15.43 to 21.34% and 79.83% and a reduction in the G1 phase fraction, from 48.83 to 41.63% and 11.52%, were observed in cells treated with amiodarone at concentrations of 0.1 and 1 mM, respectively[6].
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
NCT02814903 - Unknown August 2017 France ... 展开 >> Joachim ALEXANDRE Recruiting Caen, Basse Normandie, France, 14000 Contact: Mathieu CHEQUEL, MD    +33625342363    chequel-m@chu-caen.fr    Contact: Pierre OLLITRAULT, MD    +33624922671    ollitrault-p@chu-caen.fr 收起 <<
NCT03685149 Arrhythmogenic Right Ventricul... 展开 >>ar Cardiomyopathy 收起 << Phase 2 Not yet recruiting August 2020 United States, New York ... 展开 >> University of Rochester Medical Center Not yet recruiting Rochester, New York, United States, 14642 Contact: Spencer Rosero, MD    585-275-4775    spencer_rosero@urmc.rochester.edu    Contact: Laura Wing    585-273-4128    laura_wing@urmc.rochester.edu 收起 <<
NCT00589303 - Terminated(Lack of funding) - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.47mL

0.29mL

0.15mL

7.33mL

1.47mL

0.73mL

14.67mL

2.93mL

1.47mL
参考文献

[1]Knorre DA, Krivonosova TN, et al. Amiodarone inhibits multiple drug resistance in yeast Saccharomyces cerevisiae. Arch Microbiol. 2009 Aug;191(8):675-9.

[2]Lapenna D, Ciofani G, et al. Antioxidant activity of amiodarone on human lipoprotein oxidation. Br J Pharmacol. 2001 Jul;133(5):739-45.

[3]Lapenna D, Ciofani G, Bruno C, Pierdomenico SD, Cuccurullo F. Antioxidant activity of amiodarone on human lipoprotein oxidation. Br J Pharmacol. 2001;133(5):739-745

[4]Knorre DA, Krivonosova TN, Markova OV, Severin FF. Amiodarone inhibits multiple drug resistance in yeast Saccharomyces cerevisiae. Arch Microbiol. 2009;191(8):675-679

[5]Gray DF, Mihailidou AS, Hansen PS, et al. Amiodarone inhibits the Na(+)-K+ pump in rabbit cardiac myocytes after acute and chronic treatment. J Pharmacol Exp Ther. 1998;284(1):75-82

[6]Choi IS, Kim BS, Cho KS, et al. Amiodarone induces apoptosis in L-132 human lung epithelial cell line. Toxicol Lett. 2002;132(1):47-55