Droxicainide
(Synonyms: 羟卡尼) 目录号 : GC32525
Droxicainide是一种抗心律失常剂。
Cas No.:78289-26-6
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
Droxicainide is an antiarrhythmic agent.
In coronary artery occlusion study, Droxicainide reduces hypoperfused area that evolves to necrosis, and reduces the infarct size in dogs[1]. Droxicainide decreases the sinus node, atrial and ventricular excitability and contractile force and increases the refractoriness in the study of spontaneously beating atria, electrically stimulated atria and papillary muscles isolated from rats[2].
[1]. Faria DB, et al. Effects of lidocaine and droxicainide on myocardial necrosis: a comparative study. J Am Coll Cardiol. 1983 Jun;1(6):1447-52. [2]. Helgesen KG, et al. Comparison of electrophysiological and mechanical effects of droxicainide and lidocaine on heart muscle isolated from rats. Acta Pharmacol Toxicol (Copenh). 1984 Oct;55(4):303-7.
| Cas No. | 78289-26-6 | SDF | |
| 别名 | 羟卡尼 | ||
| Canonical SMILES | O=C(C1N(CCO)CCCC1)NC2=C(C)C=CC=C2C | ||
| 分子式 | C16H24N2O2 | 分子量 | 276.37 |
| 溶解度 | Soluble in DMSO | 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 | 3.6183 mL | 18.0917 mL | 36.1834 mL |
| 5 mM | 0.7237 mL | 3.6183 mL | 7.2367 mL |
| 10 mM | 0.3618 mL | 1.8092 mL | 3.6183 mL |
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| 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 |
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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。
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Comparison of electrophysiological and mechanical effects of Droxicainide and lidocaine on heart muscle isolated from rats
Acta Pharmacol Toxicol (Copenh) 1984 Oct;55(4):303-7.PMID:6507117DOI:10.1111/j.1600-0773.1984.tb01986.x.
A new antiarrhythmic drug, Droxicainide, was compared with lidocaine in order to evaluate Droxicainide's effect on heart muscle. Dose-response curves for electrophysiological and mechanical effects of the two drugs on spontaneously beating atria, electrically stimulated atria and papillary muscles isolated from rats were obtained. After increasing doses of both Droxicainide and lidocaine sinus node automaticity decreased, atrial and ventricular excitability and contractile force decreased and refractoriness increased. The effects of the two drugs on atrial and ventricular muscle were qualitatively and quantitatively the same, but Droxicainide was less potent. The results fit well with the concept that Droxicainide is a class 1 anti-arrhythmic drug.
Effects of lidocaine and Droxicainide on myocardial necrosis: a comparative study
J Am Coll Cardiol 1983 Jun;1(6):1447-52.PMID:6853899DOI:10.1016/s0735-1097(83)80048-5.
Lidocaine has been shown to protect ischemic myocardium, but the degree of its effectiveness is not yet well established. Therefore, in this study, the effects of this drug on ultimate infarct size were examined quantitatively. Another member of the same class of drugs, Droxicainide (ALS1249), DL-N-(2-hydroxyethyl)-pipecolinyl-2,6-dimethylanilide hydrochloride, is a new antiarrhythmic agent that has shown a good therapeutic index in the initial experimental studies. Accordingly, the effects of this drug on ultimate infarct size were examined and compared with those of lidocaine. Coronary artery occlusion was performed on 29 dogs. One minute later, technetium-99m labeled microspheres were injected into the left atrium for assessment of the hypoperfused zone (the zone at risk of infarction). Fifteen minutes after occlusion, the dogs were randomized into three groups: 9 dogs served as a control group, 10 were given lidocaine and 10 were given the same dosage of Droxicainide. Six hours after occlusion, the dogs were sacrificed and the hearts cut into 3 mm thick slices and incubated in triphenyltetrazolium chloride to delineate the area of myocardial damage. Autoradiography of the same slices provided images of the areas of myocardial hypoperfusion. Thereafter, in each dog, the percent of hypoperfused area that evolved to necrosis was calculated. In control dogs, it was 85.6 +/- 2.0%; in lidocaine-treated dogs, 68.1 +/- 4.1% (p less than 0.01), a reduction of 20%; and in droxicainide-treated dogs, 50.1 +/- 5.3%, a reduction of 41% (p less than 0.001 versus control and p less than 0.005 versus lidocaine).
Pharmacological studies on Droxicainide, a new antiarrhythmic agent
Arzneimittelforschung 1983;33(5):706-10.PMID:6683549doi
The antiarrhythmic, local anesthetic and acute local and systemic toxic effects of DL-N-(2-hydroxyethyl)-pipecolinyl-2,6-dimethylanilide (AL-S-1249, Droxicainide) and lidocaine were compared in animals. When given intravenously both substances suppressed ouabain-induced arrhythmias in pentobarbital-anesthetized guinea pigs; they were equipotent in this regard and had the same duration of antiarrhythmic action. Both substances produced generally equivalent sensory anesthesia following intradermal administration in the guinea pig and corneal application in the rabbit and block of motor and sensory function when injected near the sciatic nerve in the rat. In these local anesthetic tests and following intradermal administration to rabbits, Droxicainide produced less local tissue irritation than lidocaine. When given intravenously to unanesthetized mice and unanesthetized and pentobarbital-anesthetized rats, the LD50's for Droxicainide were consistently higher than those for lidocaine. Since Droxicainide has antiarrhythmic and local anesthetic properties that are quantitatively similar to lidocaine but local and systemic toxicity that is relatively weaker, its antiarrhythmic and local anesthetic actions merit further study.
The acute antiarrhythmic effects of Droxicainide and lidocaine in unanesthetized dogs
J Cardiovasc Pharmacol 1984 Mar-Apr;6(2):355-60.PMID:6200728DOI:10.1097/00005344-198403000-00023.
Two groups of unanesthetized dogs, each consisting of six animals with ventricular tachycardia caused by two-stage ligation of the anterior descending branch of the left coronary artery on the day before treatment, were given continuous intravenous infusions of 0.5 mg/kg/min of either Droxicainide [DL-N-(2-hydroxyethyl) pipecolinyl-2,6-dimethylanilide] hydrochloride or lidocaine hydrochloride until convulsions occurred. At low cumulative doses of either drug, the infusions produced a progressive reduction in the frequency of ventricular ectopic beats, but no significant changes in the sinus rate, the PR or QRS intervals of normal sinus beats, the arterial and central venous pressures, or the respiratory rate. At higher cumulative doses lidocaine produced sedation, and both drugs produced emesis and then convulsions that subsided soon after termination of treatment. With respect to both the cumulative doses and plasma concentrations at which they reduced the frequency of ectopic beats by 25, 50, and 75% and at which they produced convulsions, Droxicainide was a more potent antiarrhythmic agent than lidocaine and had a wider margin of safety.