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Bretylium tosylate

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Chemical Structure| 61-75-6 同义名 : 溴苄乙胺 ;Bretylium (tosylate)
CAS号 : 61-75-6
货号 : A109533
分子式 : C18H24BrNO3S
纯度 : 99%+
分子量 : 414.357
MDL号 : MFCD00038731
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(253.4 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:

PO 0.5% CMC-Na 50 mg/mL clear

生物活性
描述 Bretylium tosylate is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters. It is the sympathetic nerve and adrenergic ganglion blocking agent[3]. Bretylium reduced the velocity of hydrolysis of ACh by erythrocyte ghosts. This inhibition was competitive and the Ki of bretylium was 0.053 mM[4]. Clinical studies have shown parenteral bretylium to be effective in suppressing ventricular arrhythmias, particularly recurrent, drug resistant ventricular tachycardia or ventricular fibrillation[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.07mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL

参考文献

[1]Chandrasekaran S, Steinberg JS. Efficacy of bretylium tosylate for ventricular tachycardia. Am J Cardiol. 1999 Jan 1;83(1):115-7, A9.

[2]Kochar G, Kahn SE, Kotler MN. Bretylium tosylate and ventricular fibrillation in hypothermia. Ann Intern Med. 1986 Oct;105(4):624.

[4]Ferry CB, Norris B. Actions of bretylium tosylate at the neuromuscular junction. Br J Pharmacol. 1971 Apr;41(4):607-21. doi: 10.1111/j.1476-5381.1971.tb07069.x. PMID: 5103906; PMCID: PMC1702776.

[5]Heissenbuttel RH, Bigger JT Jr. Bretylium tosylate: a newly available antiarrhythmic drug for ventricular arrhythmias. Ann Intern Med. 1979 Aug;91(2):229-38. doi: 10.7326/0003-4819-91-2-229. PMID: 380436.