Bretylium tosylate
(Synonyms: 托西溴苄铵) 目录号 : GC30874
A class III antiarrhythmic agent
Cas No.:61-75-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bretylium is a class III antiarrhythmic agent and an inhibitor of the Na+/K+-ATPase (IC50 = 4.5 mM).1 Bretylium also has antiadrenergic activity, inhibiting auricular nerve stimulation-induced vasoconstriction in isolated rabbit ears and hypogastric nerve stimulation-induced contraction of isolated rabbit uterus.2 It inhibits neuroeffector calcium transients (NCTs), as well as increases action potential delay and the absolute refractory period, but does not inhibit field stimulus-induced CTs in isolated mouse vas deferens sympathetic nerve terminals.3 Bretylium prevents ventricular fibrillation in anesthetized dogs in a model of sudden coronary death when administered at a dose of 10 mg/kg.4 Formulations containing bretylium were previously used in the prevention and treatment of ventricular fibrillation.
1.Helms, J.B., Arnett, K.L., Gatto, C., et al.Bretylium, an organic quaternary amine, inhibits the Na,K-ATPase by binding to the extracellular K-siteBlood Cells Mol. Dis.32(3)394-400(2004) 2.Boura, A.L., Copp, F.C., and Green, A.F.New antiadrenergic compoundsNature184BA70-BA71(1959) 3.Brain, K.L., and Cunnane, T.C.Bretylium abolishes neurotransmitter release without necessarily abolishing the nerve terminal action potential in sympathetic terminalsBr. J. Pharmacol.153(4)831-839(2007) 4.Holland, K., Patterson, E., and Lucchesi, B.R.Prevention of ventricular fibrillation by bretylium in a conscious canine model of sudden coronary deathAm. Heart J.105(5)711-717(1983)
| Cas No. | 61-75-6 | SDF | |
| 别名 | 托西溴苄铵 | ||
| Canonical SMILES | C[N+](C)(CC)CC1=CC=CC=C1Br.O=S(C2=CC=C(C)C=C2)([O-])=O | ||
| 分子式 | C18H24BrNO3S | 分子量 | 414.36 |
| 溶解度 | DMSO : ≥ 30 mg/mL (72.40 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4134 mL | 12.0668 mL | 24.1336 mL |
| 5 mM | 0.4827 mL | 2.4134 mL | 4.8267 mL |
| 10 mM | 0.2413 mL | 1.2067 mL | 2.4134 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Bretylium tosylate: a review
The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects, drug interactions and dosage of bretylium tosylate, a recently approved antiarrhythmic agent, are reviewed. Bretylium tosylate is used to treat life-threatening ventricular arrhythmias, principally ventricular fibrillation and ventricular tachycardia, that have not responded to treatment with first-line antiarrhythmic agents. The drug has a direct positive inotropic effect on the myocardium and blocking effect on postganglionic sympathetic nerve transmission. The drug is poorly absorbed orally, requiring either i.m. or i.v. administration. Drug excretion occurs primarily through the kidney, necessitating dosage modification in renal disease. Hypotension is the most commonly observed adverse reaction to bretylium tosylate. Rapid i.v. administration may cause severe nausea and vomiting, and i.m. injection at the same site may cause atrophy and necrosis of muscle tissue. Quinidine and procainamide may potentiate the hypotensive effects of bretylium. Bretylium will aggravate digitalis-induced arrhythmias. Bretylium's use in resistant ventricular tachyarrhythmias requires close clinical monitoring.
Bretylium tosylate: a newly available antiarrhythmic drug for ventricular arrhythmias
Bretylium tosylate (Bretylol) has recently been approved for parenteral use against resistant ventricular arrhythmias. The pharmacologic action of bretylium is complex, and its antiarrhythmic action differs significantly from other drugs. Bretylium is an adrenergic neuronal blocking agent taken up selectively at peripheral adrenergic nerve terminals, where it initially releases norepinephrine (sympathomimetic effect) and then produces adrenergic neuronal blockade. It has direct cardiac membrane effect to prolong action potential duration and effective refractory period but, unlike other membrane active antiarrhythmic agents, does not depress conduction velocity or automaticity. Bretylium increases ventricular fibrillation threshold and prevents the decrease in ventricular fibrillation threshold associated with myocardial ischemia. It does not depress myocardial contractility. Clinical studies have shown parenteral bretylium to be effective in suppressing ventricular arrhythmias, particularly recurrent, drug resistant ventricular tachycardia or ventricular fibrillation.
Bretylium tosylate
Bretylium tosylate: profile of the only available class III antiarrhythmic agent
Bretylium tosylate, the only approved class III antiarrhythmic agent, is a unique quaternary ammonium compound with prominent experimental and clinical antifibrillatory effects. Intravenous bretylium causes a biphasic hemodynamic response; initial norepinephrine release is followed by sympathetic ganglionic blockade. Cardiac output is well maintained. Electrocardiographic intervals are unchanged, and global conduction unchanged or facilitated. With long-term experimental use, proportionate lengthening of ventricular action potential and refractory period occurs. Bretylium is largely eliminated unchanged in the urine, with a long terminal half-life of about 13 hours. Bretylium demonstrates substantial activity in several animal models and clinical circumstances of ventricular fibrillation, including those in which standard antiarrhythmic therapy is ineffective. Bretylium is thus currently approved as a first-line agent for prophylaxis and treatment of ventricular fibrillation, and as a second-line agent for ventricular tachycardia and other prefibrillatory ventricular arrhythmias. In contrast, bretylium's weak antiectopic activity and limited oral absorption make it a poor choice for management of simple ventricular ectopy. Side effects of bretylium are generally limited to its hemodynamic actions (eg, postural hypotension). Nausea may occur with rapid intravenous administration. Emerging clinical concepts emphasize the clinical importance of antifibrillatory action over antiectopic effects alone. Bretylium is thus likely to continue to find increasing usage in the acute management of malignant ventricular arrhythmia.
Bretylium tosylate enhances salt taste
Bretylium tosylate (BT), an antifibrillary drug, was found to potentiate the taste of NaCl and LiCl in both humans and rats. Application of 1 mM BT (pH 6.3) to the human tongue statistically potentiated the taste of 0.2 M NaCl and 0.2 M LiCl by 33.5% and 12.5% respectively. Electrophysiological taste responses from nucleus tractus solitarius (NTS) in rat for both hyposmotic and hyperosmotic concentrations of NaCl and 0.1 M LiCl were also increased by 30 to 40% after application of 1 mM BT. This potentiation induced by BT was reduced by amiloride in both humans and rats. Furthermore, amiloride became ineffective in inhibiting taste responses to NaCl in the presence of BT.