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G蛋白偶联受体/G蛋白
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/ 5-羟色胺受体 / Rizatriptan

Rizatriptan {[allProObj[0].p_purity_real_show]}

货号：A138654

Rizatriptan a selective 5-HT1 receptor agonist used for the treatment of migraine headaches.

Rizatriptan 化学结构 CAS号：144034-80-0
Rizatriptan 化学结构
CAS号：144034-80-0
Rizatriptan 3D分子结构
CAS号：144034-80-0
Rizatriptan 化学结构 CAS号：144034-80-0
Rizatriptan 3D分子结构 CAS号：144034-80-0
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Rizatriptan 纯度/质量文件 产品仅供科研

货号：A138654 标准纯度： {[allProObj[0].p_purity_real_show]}
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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 ✔ 98%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 98%
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 ✔ 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 98%
Fluoxetine HCl ✔ 99.5%
Paroxetine hydrochloride ✔ AChR 97%
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

 		98%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

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

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

 		99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

 		99%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

 		99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

 		98%
Tropisetron ✔ 99%
Palonosetron ✔ 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

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

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		98%
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-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 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

 		98%
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。

Rizatriptan 生物活性

描述 Rizatriptan, a quick and consistent 5-HT1B/1D agonist, is mainly used for the treatment of migraine[3]. In vitro studies, rizatriptan, with the lower maximum contractile response, would be less effective than sumatriptan in causing contraction of human isolated coronary artery[4]. Besides this, it was found that rizatriptan could not only cause about 10-fold effect of vasoconstriction in human isolated middle meningeal artery than in human coronary artery, but also more effectively promote the expression of 5-HT1B-receptors in middle meningeal artery than in coronary artery[5]. In vivo studies, rizatriptan could inhibit the expression of calcitonin gene-related peptide (CGRP) and cholecystokinin (CCK) in the rat migraine model induced by nitroglycerin, contributing to the mitigation of migraine[6]. In addition, rizatriptan, combined with inflammatory soup, has the ability of inducing nociception-related behaviours in Sprague-Dawley rats, as well as increasing Fos expression in the cortex and trigeminal pathway[7].

Rizatriptan 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
NCT00360282 - Completed - -
NCT01332500 - Completed - -
NCT01381523 - Completed - -

Rizatriptan 参考文献

[1]Perez M, Fourrier C, et al. Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors. J Med Chem. 1995 Sep 1;38(18):3602-7.

[2]Street LJ, Baker R, et al. Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl] ethylamine and analogues: potent agonists for 5-HT1D receptors. J Med Chem. 1995 May 12;38(10):1799-810.

[3]Pascual J. A review of rizatriptan, a quick and consistent 5-HT1B/1D agonist for the acute treatment of migraine. Expert Opin Pharmacother. 2004 Mar;5(3):669-77. doi: 10.1517/14656566.5.3.669. PMID: 15013934.

[4]Longmore J, Boulanger CM, Desta B, Hill RG, Schofield WN, Taylor AA. 5-HT1D receptor agonists and human coronary artery reactivity in vitro: crossover comparisons of 5-HT and sumatriptan with rizatriptan and L-741,519. Br J Clin Pharmacol. 1996 Oct;42(4):431-41. doi: 10.1046/j.1365-2125.1996.04217.x. PMID: 8904614; PMCID: PMC2042688.

[5]Longmore J, Razzaque Z, Shaw D, Davenport AP, Maguire J, Pickard JD, Schofield WN, Hill RG. Comparison of the vasoconstrictor effects of rizatriptan and sumatriptan in human isolated cranial arteries: immunohistological demonstration of the involvement of 5-HT1B-receptors. Br J Clin Pharmacol. 1998 Dec;46(6):577-82. doi: 10.1046/j.1365-2125.1998.00821.x. PMID: 9862247; PMCID: PMC1873795.

[6]Yao G, Han X, Hao T, Huang Q, Yu T. Effects of rizatriptan on the expression of calcitonin gene-related peptide and cholecystokinin in the periaqueductal gray of a rat migraine model. Neurosci Lett. 2015 Feb 5;587:29-34. doi: 10.1016/j.neulet.2014.12.021. Epub 2014 Dec 15. PMID: 25524408.

[7]Su M, Ran Y, Han X, Liu Y, Zhang X, Tan Q, Li R, Yu S. Rizatriptan overuse promotes hyperalgesia induced by dural inflammatory stimulation in rats by modulation of the serotonin system. Eur J Neurosci. 2016 Aug;44(4):2129-38. doi: 10.1111/ejn.13296. Epub 2016 Jun 28. PMID: 27288111.

Rizatriptan 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.56mL

3.71mL

1.86mL

37.13mL

7.43mL

3.71mL

Rizatriptan 技术信息

CAS号144034-80-0
分子式C15H19N5
分子量 269.345
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度
动物实验配方

Tags: Rizatriptan | 5-HT Receptor | AmBeed-信号通路专用抑制剂 | Rizatriptan 纯度/质量文件 | Rizatriptan 亚型比较 | Rizatriptan 生物活性 | Rizatriptan 临床数据 | Rizatriptan 参考文献 | Rizatriptan 实验方案 | Rizatriptan 技术信息

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