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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。 |
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]. |
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 << | |
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 |
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
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