Urapidil
产品说明书
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同义名 : | - |
| CAS号 : | 34661-75-1 | |
| 货号 : | A692483 | |
| 分子式 : | C20H29N5O3 | |
| 纯度 : | 98% | |
| 分子量 : | 387.48 | |
| MDL号 : | MFCD00133908 | |
| 存储条件： |
Pure form Sealed in dry, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Urapidil is a α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist. Urapidil does not affect vascular tone at concentrations up to 10-5 M. Urapidil (10-5 M) markedly inhibits the alpha 1-adrenergic agonist (phenylephrine)-induced concentration-dependent contractions in aortic rings without endothelium and also to some extent in those with endothelium. Moreover, the inhibitory effect of Urapidil is more pronounced in rings without endothelium than in those with endothelium[3]. It has an alpha 1-blocking action, a weak beta 1-blocking effect, an interaction with a serotonin receptor and a central depression of sympathetic tone. Urapidil is well absorbed orally with a bioavailability of about 70% and a time to peak concentration of about 4 hours after a sustained release capsule. It is metabolized in the liver at a half-life of 4.7 hours. Urapidil does not inhibit the exercise increase in heart rate[4]. Urapidil has also been shown to improve glucose and lipid metabolism in hypertensive patients with concomitant diabetes and/or hyperlipidemia[5]. Urapidil, in contrast to nicardipine and clevidipine, preserves the hypoxia-triggered vasoconstriction in isolated pulmonary arteries[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00716079 | - | Completed | - | - | |
| NCT00716079 | Intracerebral Hemorrhage ... 展开 >> Stroke Hypertension 收起 << | Not Applicable | Completed | - | - |
| NCT02795377 | - | Completed | - | Germany ... 展开 >> Division of Cardiology, Pulmonology and Vascular Medicine Duesseldorf, Duesseldorf, NRW, Germany, 40225 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.58mL 0.52mL 0.26mL |
12.90mL 2.58mL 1.29mL |
25.81mL 5.16mL 2.58mL |
| 参考文献 |
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