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Urapidil Hydrochloride CAS 34661-75-1 URA

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  • Appearance: White powder
  • Assay: 99. 0%min
  • Stock: In stock
  • Sample: Available
  • Zhishang Chemical: Urapidil Hydrochloride Supplement

Basic Info of Urapidil Hydrochloride

What is Urapidil Hydrochloride?

Urapidil is a sympathetic antihypertensive drug. It acts as α 1 – adrenoceptor antagonists and 5-HT 1A receptor agonists act. Although the initial report showed that urapidil was also a α 2 – adrenoceptor agonist, which was not confirmed in later studies, proved that it had no agonist effect in the saphenous vein of dogs and ileum of guinea pigs. With others α Unlike 1-adrenoceptor villains, urapidil does not cause response tachycardia, which may be connected to its weak β 1-adrenoceptor antagonist activity and its impact on heart vagal drive. Urapidil has actually not been approved by the US Food and drug administration, yet it is offered in Europe.

Urapidil (URA), chemical name is 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl -2,4(1H,3H)-pyrimidinedione, trade name: ebrantil (ebrantil), synonym: excellent matchi, uracil substituted by phenazine.

Its mechanism of action is to block peripheral α1 receptors to expand blood vessels, and at the same time, it can activate central 5-HT1A receptors and play a role in lowering blood pressure. , Fewer adverse reactions, no tolerance for long-term use, etc. It is mainly used for elderly hypertensive crisis, pregnancy-induced hypertension syndrome, malignant hypertension after cerebral hemorrhage, and hypertension in patients after thoracotomy. The drug of choice for the treatment of severe hypertension.

Urapidil Hydrochloride Uses

  1. Urapidil is used to prepare urapidil hydrochloride crystal. It is used in Italian emergency and intensive care departments for the diagnosis and treatment of hypertension emergencies and emergencies.
  2. Urapidil is a phenylpiperazine-substituted uracil derivative. It blocks postsynaptic adrenergic α1 receptors, excites central serotonin-1 receptors, and reduces peripheral vascular resistance. It is widely used in clinical practice. It is used for various antihypertensive treatments such as hypertensive crisis, surgical antihypertensive and prevention of blood pressure peak.
  3. Urapidil has moderate presynaptic α2 receptor excitability and weak β1 receptor blocking effect, which helps to reduce the return of blood to the heart, block the release of catecholamines, reduce the pre- and post-load of the heart, and reduce the pre- and post-load of the heart in congestive heart failure. and ischemic heart disease also have a wide range of potential application value.

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Clinical Application of Urapidil

Urapidil is a selective α-receptor blocker with both peripheral and central effects. It has been clinically used for nearly 40 years since its birth. Its main mechanism of action is as follows:

  1. Peripheral effect
    Blocks postsynaptic adrenaline α1 receptors, inhibits the vasoconstrictive effect of catecholamines; rapidly expands peripheral blood vessels, reduces peripheral vascular resistance, and thus reduces cardiac afterload; at the same time, it can dilate venules, reduce venous blood return, and reduce cardiac preload. effect. It also has a moderate excitatory effect on presynaptic α2 receptors, thereby blocking the vasoconstriction and heart rate increase caused by the release of catecholamines, reducing cardiac afterload, increasing left ventricular output, maintaining a certain tension in blood vessels, and keeping blood pressure at a low level. As for unlimited lowering. Slight β1-receptor blockade inhibits the reactive heart rate increase caused by lowering of blood pressure and reduces myocardial oxygen consumption.

  2. Central action
    It stimulates the central serotonin-1 receptor, blocks the sympathetic feedback of the medulla oblongata at the central level, reduces the activity of the sympathetic nervous system, plays a central hypotensive effect, and inhibits the reflex heart rate acceleration.
  3. Promotes vasodilation
    Urapidil can stimulate tissue cells to release a large amount of calcitonin gene-related peptide (CGRP) into the blood circulation and increase the level of blood CGRP, thereby effectively antagonizing the effect of pulmonary endothelin (ET) on vasoconstriction, adjusting the imbalance of CGRP/ET ratio, promoting Dilation of blood vessels.
  4. Other
    In addition, urapidil can effectively inhibit the release of ET in the lungs, reduce its activity, and inhibit its effect on weakening myocardial contractility.

Acute heart failure refers to a group of clinical syndromes caused by various reasons, such as sudden drop in cardiac output and sudden increase in cardiac preload and postload, among which acute left heart failure is the most common. In addition to the significant increase in circulatory resistance, insufficient tissue perfusion and other cardiovascular hemodynamic disorders, the upregulation of myocardial adrenergic α1 receptors, and the excessive secretion and release of catecholamines in acute heart failure lead to neuroendocrine disorders, which further induce arrhythmias and coronary artery contractions. , aggravating the vicious cycle of myocardial ischemia and hypoxia.

In addition to angiotensin-converting enzyme inhibitors and beta-blockers, urapidil is a potential new anti-heart failure drug that can rapidly relieve symptoms of heart failure, is safe and effective, and improves the prognosis of heart failure. The evidence is as follows:

  1. Urapidil has a good anti-congestive heart failure effect;
  2. Urapidil can well improve the cardiac function of ischemic heart failure;
  3. Urapidil can inhibit and partially reverse ventricular remodeling and improve the compliance of the cardiovascular system;
  4. Urapidil shows its own advantages when combined with insufficiency of major organs such as brain and kidney.

The application of urapidil in hypertensive crisis is relatively mature. In hypertensive crisis, urapidil has: ① Rapid onset of action, accurate and safe antihypertensive effect: blood pressure drops significantly after 5 minutes of medication, and reaches 20-30 minutes. Peak and remain stable; ② Organ protection effect: Urapidil can extensively expand the arteries and veins of pulmonary and systemic circulation, increase cardiac output, but not increase myocardial oxygen consumption, slightly increase blood flow of vital organs, and has target organ protection ③ The dose-effect relationship of urapidil is not strictly linear when the blood pressure is lowered, the blood pressure reduction effect does not increase with the increase of the dose, and the blood pressure is stable. ④ Small adverse reactions, except for nausea, dizziness and sweating caused by hypotension, no other adverse reactions have been found.

At present, the research on urapidil in blood pressure mainly focuses on the following aspects:

  1. Preoperative and intraoperative application of urapidil in pheochromocytoma removal and other operations is helpful to counteract blood pressure fluctuations caused by catecholamines, and can better control intraoperative and postoperative blood pressure without obvious hypotension.
  2. In pregnant women with pre-eclampsia and gestational hypertension, urapidil can dilate the umbilical-driven vein, does not significantly reduce the blood supply to the fetus, and has little effect on fetal accumulation, which can help pregnant women safely lower blood pressure during pregnancy.
  3. Urapidil has a certain effect of lowering intraocular pressure. Although its mechanism is still under study, it can be safely used in glaucoma patients compared with nitrates.
  4. There is no significant decrease in cerebral perfusion and no significant increase in intracranial pressure. Urapidil has advantages over calcium channel blockers and nitrates in the process of blood pressure lowering in cerebrovascular disease.

Urapidil can affect the ratio, differentiation and maturation of thymocytes CD4/CD8 cells, and its effect on humans remains to be further clarified. Experiments by Li et al. showed that urapidil has a certain effect on reducing hepatic venous wedge pressure and hepatic venous pressure gradient in liver cirrhosis. The specific mechanism of this effect remains to be further studied.

There is mature experience in the application of urapidil in cardiovascular disease, but its application in acute heart failure still lacks evidence-based medical support, most of the research results are single, small sample studies, lack of multi-center, The conclusion of the large sample study supports that most of the current research is on hemodynamic monitoring in the acute phase, but lacks the observation of the neuroendocrine impact of acute events, and the short-term and long-term prognosis of patients needs to be further clarified. For the long-term application, the drug resistance, rebound, application time and scope of long-term application, and the impact on vascular endothelial and coagulation functions still need to be further studied.

In conclusion, urapidil is a first-line drug for the treatment of hypertensive emergencies with rapid blood pressure reduction through dual mechanisms and safe use of dual-channel metabolism.

Preparation of Urapidil Hydrochloride

  • Reverse Phase Transfer Catalytic Preparation of Urapidil
    In a 500mL three-necked flask, add Na2CO3 (53.3g, 0.5mol), β-CD4.0g and 200mL water, stir until the system is clear, then add 1-(2-methoxyphenyl)piperazine hydrochloride (2 ) (57g, 0.25mol), heated to 95°C, added 6-(3-chloropropyl)amino-1,3-dimethyluracil (1) (57.3g, 0.248mol) in three batches, the addition was completed , continue the reflux reaction, TLC follows the reaction until the raw material point basically disappears, and it takes about 2~3h. Then, the reaction solution was poured into water at 50-60° C. while still hot, stirred and cooled to room temperature, and a white solid was precipitated, filtered, and dried to obtain 80.0 g of the product with a yield of 83.4% and a purity of 97.8%.乌拉地尔的合成路线
  • Purification of urapidil by anti-solvent recrystallization
    Add 40 g of urapidil with a purity of more than 96% into 200 mL of dichloromethane, heat to dissolve, and suction filtration while hot, and then quickly pour the obtained filtrate into 1200 mL of acetone at a stirring speed of 1500 r?min?1. Crystallize at a temperature of ℃, collect the precipitated white powder, and dry to obtain 37.0 g of an anti-solvent recrystallized product with a yield of more than 95.0% and a purity of more than 98.5%.

Reference

  1. Urapidil – PubChem
  2. Ramage AG (April 1991). “The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors”Br. J. Pharmacol
  3. Tan Shaoling, Xue Xiuqing, Xiao Xiaoyan, Huang Shaohua.Clinical application and research progress of urapidil[J].Journal of Guangdong University of Pharmacy,2001(01):28-31.

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