Pronethalol ((±)-Pronethalo)
(Synonyms: 丙萘洛尔; (±)-Pronethalo) 目录号 : GC32538
Pronethalol ((±)-Pronethalo) ((±)-Pronethalo) 是一种非选择性的 β-肾上腺素能拮抗剂。
Cas No.:54-80-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pronethalol is a non-selective beta-adrenergic blocking agent, protect against and to reverse Digitalis-induced ventricular arrhythmias. Target: beta-adrenergic receptor
[1]. Aroesty JM, et al. The effects of a beta-adrenergic blocking agent, pronethalol, on digitalis-induced ventricular arrhythmias. Am Heart J. 1966 Apr;71(4):503-508.
| Cas No. | 54-80-8 | SDF | |
| 别名 | 丙萘洛尔; (±)-Pronethalo | ||
| Canonical SMILES | OC(CNC(C)C)C1=CC=C2C=CC=CC2=C1 | ||
| 分子式 | C15H19NO | 分子量 | 229.32 |
| 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 | 4.3607 mL | 21.8036 mL | 43.6072 mL |
| 5 mM | 0.8721 mL | 4.3607 mL | 8.7214 mL |
| 10 mM | 0.4361 mL | 2.1804 mL | 4.3607 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。
THE EFFECTS OF Pronethalol, DICHLOROISOPRENALINE AND DISOPYRAMIDE ON THE TOXICITY TO THE HEART OF OUABAIN AND ANAESTHETICS
Br J Pharmacol Chemother 1963 Dec;21(3):462-72.PMID:14110746DOI:10.1111/j.1476-5381.1963.tb02014.x.
An intermittent infusion of ouabain, 4 mug during 30 sec every 1.5 min, regularly caused ventricular fibrillation in guinea-pigs. The beta-receptor blocking drug, Pronethalol (5 mg/kg), increased the dose of ouabain required to produce extrasystoles, completely prevented fibrillation, and significantly raised the lethal dose of ouabain. Dichloroisoprenaline had similar effects, but a dose of 15 mg/kg was required. When fibrillation had already been produced by ouabain, Pronethalol (3 to 4 mg) administered slowly restored a regular rhythm, but rapid injection sometimes produced cardiac arrest. As much as 20 to 25 mg/kg of Pronethalol could be given to animals deeply anaesthetized with urethane or pentobarbitone, but with light chloroform or ether anaesthesia, 5 mg/kg of Pronethalol caused a large fall in blood pressure and complete heart-block.
A COMPARISON OF THE ANTIFIBRILLATORY ACTIONS AND EFFECTS ON INTRACELLULAR CARDIAC POTENTIALS OF Pronethalol, DISOPYRAMIDE AND QUINIDINE
Br J Pharmacol Chemother 1963 Dec;21(3):473-81.PMID:14110747DOI:10.1111/j.1476-5381.1963.tb02015.x.
A quantitative comparison of the effects of quinidine, Pronethalol and gamma-di-isopropylamino-alpha-phenyl-alpha-pyrid-2-ylbutyramide (disopyramide) has been made on rabbit isolated atria. All three drugs raised the electrical threshold and reduced the contractions, the conduction velocity and the maximal frequency at which the atria would follow a stimulus. The descending order of potency was Pronethalol, quinidine and disopyramide, but the range was small, Pronethalol having about twice the activity of disopyramide. Both the new compounds affected intracellular potentials in the same way as quinidine, causing little change in the resting potential or duration of the action potential, but reducing the overshoot potential and slowing the rate of rise of the action potential. These results support the view that interference with depolarization is an essential feature of antifibrillatory activity.
Reversal by Pronethalol of dibenamine blockade: a study on the seminal vesicle of the guinea-pig
Br J Pharmacol 1969 Jul;36(3):594-601.PMID:4389284DOI:10.1111/j.1476-5381.1969.tb08014.x.
1. The guinea-pig seminal vesicle has been shown to be a very suitable test object for the study of mechanisms involving alpha-adrenoceptive receptors, because no beta-receptors were found in this preparation.2. Adrenaline, noradrenaline and phenylephrine were directly acting agonists, their ED50 values being 7.1 x 10(-6)M, 1.5 x 10(-5)M and 2.7 x 10(-5)M, respectively.3. Pretreatment with reserpine had no influence on the contractions caused by adrenaline, noradrenaline and phenylephrine but abolished or greatly reduced the contractions caused by dopamine. Cocaine enhanced the effects of adrenaline, noradrenaline and phenylephrine and reduced those of dopamine.4. Pronethalol (6.8 x 10(-5)M) reversed the alpha-receptor blockade by dibenamine, ergotamine and phentolamine of responses to adrenaline, noradrenaline and phenylephrine; it did not affect the blockade by dibenamine of responses to histamine.5. Reversal of the blockade by dibenamine was observed only when its concentration was such that it caused a parallel shift of the dose-effect curves of the agonists to the right; higher concentrations, which caused an unsurmountable depression of the maximal contraction, were not antagonized by Pronethalol.6. It is assumed that the reversal is dependent on a direct action on alpha-receptors, "spare receptors" being probably involved.
Improved enantiospecific RP-HPLC assays for propranolol in plasma and urine with Pronethalol as internal standard
J Anal Toxicol 1991 Jul-Aug;15(4):209-13.PMID:1682529DOI:10.1093/jat/15.4.209.
For the enantiospecific assay of propranolol in biological material, formation of diastereomeric derivatives is one possible approach. The aim of the present study was the development and optimization of three analytical methods based on different chiral reagents: phenylethylisocyanate and the acyl chloride as well as the isocyanate that are derived from the fluorescent S-flunoxaprofen. Pronethalol is used as internal standard in all three procedures and improves the coefficients of variation significantly. After extraction from human plasma or urine, propranolol is reacted with one of these compounds in anhydrous organic solvents with addition of triethylamine. The diastereomeric derivatives are then resolved on an octadecylsilane column using mixtures of water and methanol with or without addition of glacial acetic acid. Good resolutions of the diastereomeric derivatives are found under these conditions. Conjugates are cleaved prior to analysis using beta-glucuronidase-arylsulfatase and assayed as parent propranolol enantiomers. All three procedures were suitable for analysis of propranolol enantiomers in biological samples in the lower nanogram range (1-2 ng/mL). A preliminary clinical study confirmed the known enantiospecificity in the pharmacokinetics of propranolol and showed high concentrations of conjugates with R/S ratios that were similar to those of the parent enantiomers.