Cibenzoline
(Synonyms: 西苯唑啉,Cifenline; Ro 22-7796) 目录号 : GC64925
Cibenzoline 是一种有效的 KATP 通道抑制剂，直接影响成孔的 Kir6.2 亚基而不是 SUR1 亚基。Cibenzoline 是 Ia 类抗心律失常药物。Cibenzoline 几乎没有抗胆碱能活性。Cibenzoline 显着减弱 LVPG，与心肌收缩力下降有密切关系。Cibenzoline 具有用于肥厚型梗阻性心肌病研究的潜力。
Cas No.:53267-01-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic drug. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy[1][2].
[1]. Mukai E, et al. The antiarrhythmic agent cibenzoline inhibits KATP channels by binding to Kir6.2. Biochem Biophys Res Commun. 1998;251(2):477-481.
[2]. Hamada M, et al. Class Ia antiarrhythmic drug cibenzoline: a new approach to the medical treatment of hypertrophic obstructive cardiomyopathy. Circulation. 1997;96(5):1520-1524.
| Cas No. | 53267-01-9 | SDF | Download SDF |
| 别名 | 西苯唑啉,Cifenline; Ro 22-7796 | ||
| 分子式 | C18H18N2 | 分子量 | 262.35 |
| 溶解度 | DMSO : 100 mg/mL (381.17 mM; ultrasonic and warming and heat to 60°C) | 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 | 3.8117 mL | 19.0585 mL | 38.117 mL |
| 5 mM | 0.7623 mL | 3.8117 mL | 7.6234 mL |
| 10 mM | 0.3812 mL | 1.9059 mL | 3.8117 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。
Cibenzoline. A review of its pharmacological properties and therapeutic potential in arrhythmias
Drugs 1992 May;43(5):734-59.PMID:1379150DOI:10.2165/00003495-199243050-00008.
Cibenzoline is a class I antiarrhythmic drug with limited class III and IV activity which can be administered orally or intravenously. An elimination half-life of about 8 to 12 hours permits twice daily administration, although age and renal function must be considered when determining dosage. Cibenzoline has some activity in ventricular and supraventricular arrhythmias, including drug-refractory ventricular tachycardia or ventricular arrhythmias following recent acute myocardial infarction, although results in patients with sustained ventricular tachycardia are less promising. In comparative trials, Cibenzoline has demonstrated efficacy similar to or better than that of a variety of other class I antiarrhythmic drugs and was at least as well tolerated, with a more convenient dosage schedule. However, further studies to clarify the proarrhythmic effects of Cibenzoline and its use in patients with impaired left ventricular function are required, and the use of Cibenzoline (and other class I antiarrhythmic agents) in patients with other than potentially lethal ventricular arrhythmias should be avoided following the results of the CAST studies. Thus, Cibenzoline is an effective antiarrhythmic agent with a favourable pharmacokinetic profile that may be considered with other class I drugs in patients requiring therapy for high risk arrhythmias.
[A case of myasthenia-like symptoms induced by Cibenzoline overdosage]
Rinsho Shinkeigaku 2018 Jan 26;58(1):41-44.PMID:29269691DOI:10.5692/clinicalneurol.cn-001070.
The present patient was an 87-year-old man who had been taking Cibenzoline for tachyarrhythmia. Five years after initiation of administration, he was referred to our hospital for ptosis that worsened from midday, as well as weakness of the facial and limb muscles. He tested negative for anti-acetylcholine receptor antibody but positive in the edrophonium test, suggesting that he had myasthenia gravis. He was admitted to our hospital 3 years later due to worsening symptoms of ptosis and muscle weakness. He had hypoglycemia, cardiac conduction defect, and renal dysfunction. In addition, blood concentration of Cibenzoline was markedly high (1,850 ng/ml). We terminated the administration of Cibenzoline, after which the patient's neurologic symptoms improved. Our findings suggest that Cibenzoline toxicity must be considered in differentiating myasthenia gravis when a patient also presents with renal dysfunction.
Efficacy of Cibenzoline for hypertrophic obstructive cardiomyopathy in paediatric patients with RAS/MAPK pathway syndromes
Cardiol Young 2022 Oct 12;1-3.PMID:36221307DOI:10.1017/S1047951122003183.
RASopathies - caused by mutations in the RAS/MAPK signaling pathway - are frequently associated with cardiac diseases, such as hypertrophic obstructive cardiomyopathy. Although Cibenzoline is useful for adult hypertrophic obstructive cardiomyopathy patients, little is known about its effect in children. Here, we report two paediatric cases of hypertrophic obstructive cardiomyopathy associated with RASopathies where the condition was improved by Cibenzoline.
[Cibenzoline]
Arch Mal Coeur Vaiss 1985 Oct;78 Spec No:91-4.PMID:3938265doi
Cibenzoline is an imidazoline derivative with antiarrhythmic properties. It is rapidly absorbed after oral administration. The bio-availability is nearly 100%. The drug half-life is between 4 and 7 hours. The drug depresses left ventricular contraction and increases systemic vascular resistance. Cibenzoline has been shown to decrease the maximal rate of rise of depolarisation in isolated cardiac fibers. The duration of action potential is increased. Voltage-clamp studies have shown a reduction in the fast sodium and in the slow currents. The following clinical electrophysiological effects have been observed: an increase in QRS duration, in AH and HV intervals and in the effective ventricular refractory period. This compound has been shown to be effective in preventing atrial arrhythmias, in suppressing reciprocating intranodal tachycardias and tachycardias associated with the Wolff-Parkinson-White syndrome and in the treatment of ventricular arrhythmias (especially extrasystoles and non-sustained ventricular tachycardia). Side effects are rare.
Profiles of aprindine, Cibenzoline, pilsicainide and pirmenol in the framework of the Sicilian Gambit. The Guideline Committee for Clinical Use of Antiarrhythmic Drugs in Japan (Working Group of Arrhythmias of the Japanese Society of Electrocardiology)
Jpn Circ J 1999 Jan;63(1):1-12.PMID:10084381DOI:10.1253/jcj.63.1.
The Vaughan Williams classification has been used widely by clinicians, cardiologists and researchers engaged in antiarrhythmic drug development and testing in many countries throughout the world since its initial proposal in the early 1970s. However, a major criticism of the Vaughan Williams system arose from the extent to which the categorization of drugs into classes I-IV led to oversimplified views of both shared and divergent actions. The Sicilian Gambit proposed a two-dimensional tabular framework for display of drug actions to solve these problems. From April to December 1996, members of the Guideline Committee met to discuss pharmacologic profiles of 4 antiarrhythmic drugs (aprindine, Cibenzoline, pilsicainide, and pirmenol) that were not included in the original spreadsheet but are used widely in clinical practice in Japan. The discussion aimed to fit the drug profiles into the Gambit framework based on all the important literature published to date regarding the actions of the 4 drugs. This report is a summary of that deliberation.