Tocainide hydrochloride
(Synonyms: N-(2-氨基丙酰基)-2,6-二甲基苯胺) 目录号 : GC38865
Tocainide hydrochloride 是一种 sodium channel 阻滞剂，在产生疼痛的病灶中(神经膜上) 阻断钠通道。Tocainide hydrochloride 是利多卡因 (lignocaine) 的一种伯胺类似物，用于治疗心律不齐。
Cas No.:71395-14-7
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
Tocainide hydrochloride is a sodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus[1][2].
Tocainide (100 mg/kg) effectively suppresses ventricular ectopic activity in unanesthetized dogs with coronary occlusion. Termination of tocainide infusion in both digitalis toxicity and coronary occlusion models results in prompt return of ventricular ectopic activity[1].
[1]. Alpert JS, et al. Chemistry, pharmacology, antiarrhythmic efficacy and adverse effects of tocainide hydrochloride, an orally active structural analog of lidocaine. Pharmacotherapy. 1983 Nov-Dec;3(6):316-23. [2]. De Luca A,et al.Optimal requirements for high affinity and use-dependent block of skeletal muscle sodium channel by N-benzyl analogs of tocainide-like compounds.Mol Pharmacol. 2003 Oct;64(4):932-45.
| Cas No. | 71395-14-7 | SDF | |
| 别名 | N-(2-氨基丙酰基)-2,6-二甲基苯胺 | ||
| Canonical SMILES | CC(N)C(NC1=C(C)C=CC=C1C)=O.[H]Cl | ||
| 分子式 | C11H17ClN2O | 分子量 | 228.72 |
| 溶解度 | DMSO : 125 mg/mL (546.52 mM; Need ultrasonic); H2O : 50 mg/mL (218.61 mM; Need ultrasonic) | 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 | 4.3722 mL | 21.8608 mL | 43.7216 mL |
| 5 mM | 0.8744 mL | 4.3722 mL | 8.7443 mL |
| 10 mM | 0.4372 mL | 2.1861 mL | 4.3722 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。
Chemistry, pharmacology, antiarrhythmic efficacy and adverse effects of Tocainide hydrochloride, an orally active structural analog of lidocaine
Pharmacotherapy 1983 Nov-Dec;3(6):316-23.PMID:6419205DOI:10.1002/j.1875-9114.1983.tb03286.x.
Tocainide is an orally effective antiarrhythmic agent, structurally and pharmacologically similar to lidocaine. It appears to be free of marked negative hemodynamic or electrophysiologic effects in patients with heart disease, despite a high frequency of minor and often transient central nervous system and gastrointestinal side effects. Tocainide is effective in suppressing ventricular arrhythmias in a variety of settings. This agent may be a useful addition to our antiarrhythmic armamentarium.
Treatment of tinnitus with Tocainide hydrochloride
Otolaryngol Head Neck Surg 1980 Jul-Aug;88(4):442-6.PMID:6821429doi
Intravenous (IV) injection of lidocaine was used in patients with tinnitus for combined treatment with oral anticonvulsants carbamazepine (Tegretol) and primidone (Mysoline). In most cases, the high complication rate with these drugs precluded their long-term use. Tocainide hydrochloride (HCl), a primary amine analog of lidocaine, can be taken orally and was evaluated for the use in the treatment of tinnitus. A double-blind study in which one group received 200 mg tocainide HCl four times a day and one group received a placebo revealed no significant differences in tinnitus relief between the two groups. A single-blind study in which 600 mg tocainide HCl four times a day was administered showed 80% to 98% tinnitus relief in five of the six patients who tolerated the drug. Tocainide HCl treatment of tinnitus is promising.
Metabolism of tocainide in the rat
J Pharm Sci 1982 May;71(5):491-4.PMID:6808112DOI:10.1002/jps.2600710504.
The metabolism of tocainide, an oral antiarrhythmic agent, was studied in male Wistar rats following oral administration of 15 mg/kg of Tocainide hydrochloride. Qualitative and quantitative identification of the metabolites in urine was carried out by GC-mass spectrometry and electron capture detector gas chromatography. About 15-20% of the dose administered was excreted as intact drug in the urine. An additional 20% of the dose was present as acid hydrolysable conjugates. Enzymatic hydrolysis (beta-glucuronidase) revealed half of the acid hydrolysable conjugates to be a glucuronide. The enzyme mediated hydrolysis was blocked by its specific inhibitor saccharo-1,4-lactone. N-acetyl tocainide, an oxidatively deaminated tocainide, an aldehyde adduct of tocainide, and a cyclic hydantoin derivative of tocainide were also identified as metabolites in the urine samples.
A sequential double blind cross-over trial of Tocainide hydrochloride in tinnitus
Clin Otolaryngol Allied Sci 1985 Apr;10(2):97-101.PMID:3928215DOI:10.1111/j.1365-2273.1985.tb01175.x.
A sequential double blind cross-over trial of Tocainide hydrochloride, an oral analogue of lignocaine, is reported. The dosage of Tocainide hydrochloride ranged from 200-600 mg daily. Of the 32 patients who completed the trial, 1 had complete relief and 2 had partial relief of their tinnitus whilst taking tocainide. An increased incidence of side-effects in patients taking tocainide was noted, in particular, headache, dizziness, nausea and skin rashes.