Dopropidil
(Synonyms: 多普吡地) 目录号 : GC32652
Dopropidil是一种新型的抗心绞痛钙离子调节剂，具有细胞内钙拮抗剂活性，在动物模型中具有抗缺血活性作用。
Cas No.:79700-61-1
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
Animal experiment: | Rabbits[1] Groups of rabbits given a normal diet or one containing Cholesterol (1 %) are treated with vehicle, Diltiazem (10 mg/kg per day,p.o.), or Dopropidil (30 mg/kg per day, p.o.) over a 14-week period. Animals are then killed and certain blood vessels examined macroscopically, microscopically, and pharmacologically for reactivity to certain vasoactive agents. |
References: [1]. J. Planellas, et al. Dopropidil, A Novel Antianginal Calcium Modulating Agent. Cardiovascular Drug Reviews. Vol.12, No.3, pp. 208-224. | |
Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity andanti-ischemic effects in several predictive animal models.
Dopropidil is able to inhibit caffeine-induced contractions of rabbit renal arteries in a calcium-free medium (IC50=30.0 uM). Dopropidil inhibits norepinephnne (NE)-induced responses with IC50s of 2.7 and 29.8 uM, respectively. At 3 and 10 μM, Dopropidil significantly reduces the maximum increase in diastolic tension evoked by veratrine (IC50=2.8 μM)[1].
Dopropidil (1 and 2.5 mg/kg) dose-dependently reduces the electrical (ST segment elevation), biochemical (lactate production and potassium release), and mechanical (loss in myocardial segment contractility) perturbations induced by ischemia in the anesthetized dog. Intraduodenal administration of Dopropidil (50 mg/kg) significantly reduces isoproterenol-induced tachycardia. This effect is manifest at 15-120 min following administration of the compound which indicates a rapid absorption and a long duration of action. In conscious dogs Dopropidil (12-14 mg/kg p.o.) reduces resting heart rate by approximately10 beats/min[1].
[1]. J. Planellas, et al. Dopropidil, A Novel Antianginal Calcium Modulating Agent. Cardiovascular Drug Reviews. Vol.12, No.3, pp. 208-224.
| Cas No. | 79700-61-1 | SDF | |
| 别名 | 多普吡地 | ||
| Canonical SMILES | CC#CC1(OCC(N2CCCC2)COCC(C)C)CCCCC1 | ||
| 分子式 | C20H35NO2 | 分子量 | 321.5 |
| 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 | 3.1104 mL | 15.5521 mL | 31.1042 mL |
| 5 mM | 0.6221 mL | 3.1104 mL | 6.2208 mL |
| 10 mM | 0.311 mL | 1.5552 mL | 3.1104 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。
Electrophysiologic effects of ORG 30701 (Dopropidil) on rabbit ventricular myocardium
J Cardiovasc Pharmacol 1993 Feb;21(2):310-5.PMID:7679167DOI:10.1097/00005344-199302000-00018
The electrophysiologic effects of ORG 30701 (1-8 x 10(-6) M) were tested in a thin, two-dimensional sheet of ventricular myocardium. Special attention was paid to a possible promotion of reentrant excitation. The drug did not increase the degree of inhomogeneity of conduction and because of the marked effect on refractoriness prevent fast rates (either spontaneously or driven). If the extracellular potassium concentration was lowered (from 5.6 to 2.0 mM), the enhancement of refractoriness by the drug was more marked. The changes in refractoriness do not appear to be based on lengthening of the repolarization of the action potential, but rather on post-repolarization refractoriness; therefore, the occurrence of triggered activity (early afterdepolarizations) is not anticipated. ORG 30701 is a cardioactive drug that because of its calcium antagonistic action acts as an antianginal drug and, in addition, exhibits antiarrhythmic properties.