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Urapidil/乌拉地尔 {[allProObj[0].p_purity_real_show]}

货号:A692483

Urapidil is a sympatholytic antihypertensive drug.

Urapidil/乌拉地尔 化学结构 CAS号:34661-75-1
Urapidil/乌拉地尔 化学结构
CAS号:34661-75-1
Urapidil/乌拉地尔 3D分子结构
CAS号:34661-75-1
Urapidil/乌拉地尔 化学结构 CAS号:34661-75-1
Urapidil/乌拉地尔 3D分子结构 CAS号:34661-75-1
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Urapidil/乌拉地尔 纯度/质量文件 产品仅供科研

货号:A692483 标准纯度: {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

98%
Venlafaxine 99%
Fluvoxamine maleate 99%
Iloperidone 99%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 99%
Fluoxetine HCl 99.5%
Paroxetine HCl AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

95%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

98%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

98%
Tropisetron 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron HCl dihydrate 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Urapidil/乌拉地尔 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].

Urapidil/乌拉地尔 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 <<

Urapidil/乌拉地尔 参考文献

[1]Ramage AG. The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors. Br J Pharmacol. 1991 Apr;102(4):998-1002.

[2]Eltze M. Investigations on the mode of action of a new antihypertensive drug, urapidil, in the isolated rat vas deferens. Eur J Pharmacol. 1979 Oct 26;59(1-2):1-9.

[3]Bopp C, Auger C, Diemunsch P, Schini-Kerth V. The effect of urapidil, an alpha-1 adrenoceptor antagonist and a 5-HT1A agonist, on the vascular tone of the porcine coronary and pulmonary arteries, the rat aorta and the human pulmonary artery. Eur J Pharmacol. 2016 May 15;779:53-8

[4]Prichard BN, Tomlinson B, Renondin JC. Urapidil, a multiple-action alpha-blocking drug. Am J Cardiol. 1989 Aug 15;64(7):11D-15D

[5]Buch J. Urapidil, a dual-acting antihypertensive agent: Current usage considerations. Adv Ther. 2010 Jul;27(7):426-43

[6]Bopp C, Auger C, Mebazaa A, Joshi GP, Schini-Kerth VB, Diemunsch P. Urapidil, but not dihydropyridine calcium channel inhibitors, preserves the hypoxic pulmonary vasoconstriction: an experimental study in pig arteries. Fundam Clin Pharmacol. 2019 Oct;33(5):527-534

Urapidil/乌拉地尔 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.58mL

0.52mL

0.26mL

12.90mL

2.58mL

1.29mL

25.81mL

5.16mL

2.58mL

Urapidil/乌拉地尔 技术信息

CAS号34661-75-1
分子式C20H29N5O3
分子量 387.48
SMILES Code O=C1N(C)C(C=C(NCCCN2CCN(C3=CC=CC=C3OC)CC2)N1C)=O
MDL No. MFCD00133908
别名
运输蓝冰
InChI Key ICMGLRUYEQNHPF-UHFFFAOYSA-N
Pubchem ID 5639
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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