Practolol
(Synonyms: 普拉洛尔) 目录号 : GC61789
Practolol是一种有效和选择性的β1肾上腺素能受体拮抗剂。Practolol可用于心律失常的研究。
Cas No.:6673-35-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias[1][2][3].
Practolol (10 μM; 30 min) preferentially antagonizes the relaxant effects produced by R0363 in spontaneously contracted tracheal preparations from the guinea-pig[1].Practolol (10 nM-100 μM) blocks the progesterone production induced by (-)epinephrine in a dose-dependent manner in granulosa cells[2].
Practolol (0.5 mg/kg; i.v.) decreases heart rate, left ventricular dP/dt max, myocardial blood flow and cardiac output in intact close-chest dogs[3].Practolol (0.5 mg/kg; i.v.) decreases normal myocardial blood flow but flow in the ischaemic area remains unchanged after coronary artery ligation[3].
[1]. Iakovidis D, et, al. In vitro activity of RO363, a beta1-adrenoceptor selective agonist. Br J Pharmacol. 1980 Apr;68(4):677-85. [2]. Adashi EY, et, al. Stimulation of beta 2-adrenergic responsiveness by follicle-stimulating hormone in rat granulosa cells in vitro and in vivo. Endocrinology. 1981 Jun;108(6):2170-8. [3]. Marshall RJ, et, al. Comparative effects of propranolol and practolol in the early stages of experimental canine myocardial infarction. Br J Pharmacol. 1976 Jun;57(2):295-303.
| Cas No. | 6673-35-4 | SDF | |
| 别名 | 普拉洛尔 | ||
| Canonical SMILES | CC(NC1=CC=C(OCC(O)CNC(C)C)C=C1)=O | ||
| 分子式 | C14H22N2O3 | 分子量 | 266.34 |
| 溶解度 | DMSO: 100 mg/mL (375.46 mM) | 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 | 3.7546 mL | 18.773 mL | 37.546 mL |
| 5 mM | 0.7509 mL | 3.7546 mL | 7.5092 mL |
| 10 mM | 0.3755 mL | 1.8773 mL | 3.7546 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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| % DMSO % % Tween 80 % saline | ||||||||||
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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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Practolol metabolism in various small animal species
Xenobiotica 1979 Jul;9(7):453-8.PMID:115161DOI:10.3109/00498257909038750.
1. The metabolism of the beta-adrenergic blocking agent Practolol has been studied in a variety of small animal species, using both ring- and acetyl-14C-labelled material. After oral dosing at 100 mg/kg, elimination of 14C in urine and expired air was monitored, and urinary metabolite patterns were examined by t.l.c. 2. Marmoset was unusual in extensively deacetylating Practolol (c. 57% dose). Urinary elimination was low, with only 25% being recovered in 4 days; over 30% of urinary 14C was present as desacetyl Practolol, whereas less than 50% was unchanged Practolol. 3. Hamster was also atypical, in its extensive hydroxylation of Practolol. Urine contained 60% dose; 11% of urinary radioactivity was present as 3-hydroxypractolol, much of the polar material present (48%) appeared to be a conjugate of this, and only 35% was present as Practolol. 4. For the other species studied (rat, mouse, guinea-pig and rabbit, metabolism was more limited. Deacetylation was typically about 5%, but was somewhat higher in the mouse (8--14%). Urine was the major route of elimination and Practolol represented 50--90% of urinary radioactivity. 5. Despite extensive toxicity studies, both in species which metabolize Practolol similarly to man and in species such as the hamster and marmoset which metabolize Practolol extensively, no animal model has been found for the human adverse reactions.
Practolol: aspects of its metabolism and ocular binding in the hamster
Xenobiotica 1986 Jun;16(6):567-73.PMID:3751112DOI:10.3109/00498258609043545.
The metabolism and ocular binding of Practolol were investigated after oral administration of 14C-practolol to hamsters treated with three modifiers of mixed-function oxidase activity: piperonyl butoxide, cobalt chloride or phenobarbitone. The major urinary metabolites of Practolol were 3-hydroxypractolol and polar metabolites which included glucuronide conjugates. A number of unidentified metabolites constituted a minor portion of urinary radioactivity. Each pretreatment modified both the urinary excretion pattern (0-24 h) of Practolol and its metabolites and also the metabolite profile of eye extracts 24 h after an oral dose. None of the modifiers of mixed-function oxidase activity had any significant effect on the ocular binding (both extractable and non-extractable components) of Practolol and its metabolites. The results indicated that the non-extractable component was neither Practolol nor 3-hydroxypractolol.
Practolol-induced autoantibodies and their relation to oculo-cutaneous complications
Postgrad Med J 1977 Feb;53(616):75-7.PMID:141660DOI:10.1136/pgmj.53.616.75.
Tissue auto-antibodies were investigated in fifty-one patients (twenty-five female, twenty-six male) receiving Practolol for ischaemic heart disease or dysrhythmias and compared with those found in 204 patients (fifty-eight female, 146 male) with ischaemic heart disease who did not receive Practolol. Antinuclear factor (ANF) was found in 24% female and 16% male patients receiving Practolol, but only in 5% of female and 4% of male patients who were not taking Practolol. Thyroid cytoplasmic antibody (TCA) was detected in 16% female and 20% of male patients receiving Practolol, compared to 10% of females and 6% of males in the control group. The incidence of ANF and TCA was significantly higher (P less than 0-05) in patients receiving Practolol compared to the control group. The occurrence of gastric parietal cell antibody (PCA) and smooth muscle antibody (SMA) was not associated with Practolol therapy (odds ratio of 2-4 and 1-9 respectively). The incidence of skin and eye complications was found to be 10% and the female to male ratio of this complication was 4 : 1. The correlation between autoantibody production and oculo-cutaneous complications could not be established in such a small group but three of the patients with the complications were found to have PCA, although PCA was found not to be associated with Practolol therapy. Four of the five patients with the complications did not have circulating ANF.
Practolol in acute myocardial infarction
Acta Med Scand Suppl 1976;587:213-9.PMID:130058DOI:10.1111/j.0954-6820.1976.tb05884.x.
A double blind trial of Practolol in coronary heart disease has been conducted for 2 years. In 298 patients with acute myocardial infarction there was no reduction in overall mortality. In a group with initial heart rate over 100 per minute mortality was significantly lowered up to 1 year. Of 484 patients with coronary heart disease treatment for 2 years did not produce a significant reduction in infarction or sudden death. Beta-adrenergic blocking drugs have been shown to reduce left ventricular work and to have an antiarrhythmic action. On these grounds they would seem theoretically to have a place in the management of acute myocardial infarction. Practolol is a cardio-selective beta-blocking agent with an intrinsic sympathomimetic action, but devoid of local anaesthetic effect. It has been found effective in post infarction arrhythmias (1). In early infarction it reduces the area of necrosis as measured by surface ST segment mapping (2).
Practolol and its metabolites: tissue localization and retention in the hamster
J Pharmacol Exp Ther 1985 Aug;234(2):485-90.PMID:4020682doi
The disposition of [14C]Practolol and its tissue association in the male Syrian hamster were investigated after p.o. administration. After an acute dose of 400 mg/kg, there was a marked persistence in the eye of total radioactivity (primarily Practolol; approximate T 1/2 = 7 days) and nonextractable radioactivity which showed minimal decay over 7 days. Nonextractable radioactivity was also found in other tissues (liver, skin, small intestine and skeletal muscle examined). The level of total and nonextractable radioactivity was linearly related to dose (800 mg/kg highest dose examined). There was a marked accumulation of total and nonextractable radioactivity in the eye (7- and 14-fold, respectively) and skin (6- and 7-fold) after daily administration of 400 mg/kg for 22 days. The association of Practolol metabolites with tissue macromolecules might explain the immunological changes in patients with the practolol-induced oculomucocutaneous syndrome. The adverse effects of Practolol in humans have not yet been reproduced in any laboratory species and so the results must be interpreted with caution in relation to the toxicity of compound.