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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 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

5-羟色胺受体亚型比较

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 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 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, 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%
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-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 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-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		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

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	-	-
NCT01332500	-		Completed	-	-
NCT00910689	-		Completed	-	-
NCT00910689	Migraine Headache	Phase 4	Completed	-	United States, Ohio ... 展开 >> Ohio University Athens, Ohio, United States, 45701 OrthoNeuro, Inc. Westerville, Ohio, United States, 43081 收起 <<
NCT01381497	-		Completed	-	-
NCT01435941	-		Completed	-	-
NCT01086358	Workplace Migraine Treatment	Phase 4	Completed	-	United States, Ohio ... 展开 >> Cleveland Clinic, 9500 Euclid Avenue, C-21 Cleveland, Ohio, United States, 44195 收起 <<
NCT00246337	-		Completed	-	-
NCT02670161	Brain Tumors ... 展开 >>Epilepsy Migraine Mild Cognitive Impairment Concussion Multiple Sclerosis Neuropathy Parkinson's Restless Legs Syndrome Stroke 收起 <<	Phase 4	Enrolling by invitation	April 2020	-
NCT00443209	Migraine	Phase 3	Completed	-	-
NCT00246337	Migraine	Phase 2	Completed	-	-
NCT00443209	-		Completed	-	-
NCT00092963	Migraine	Phase 3	Completed	-	-
NCT00095004	Migraine	Phase 3	Completed	-	-
NCT01086358	-		Completed	-	-
NCT00250458	Migraine	Phase 3	Completed	-	-
NCT00111722	Migraine	Phase 3	Completed	-	-
NCT00632385	Migraine	Phase 4	Completed	-	United States, California ... 展开 >> Pfizer Investigational Site Irvine, California, United States, 92618 Pfizer Investigational Site Newport Beach, California, United States, 92660-2452 Pfizer Investigational Site San Francisco, California, United States, 94109 United States, Florida Pfizer Investigational Site Plantation, Florida, United States, 33324 Pfizer Investigational Site St Petersburg, Florida, United States, 33710 Pfizer Investigational Site Tampa, Florida, United States, 33609 United States, Georgia Pfizer Investigational Site Marietta, Georgia, United States, 30067 United States, Indiana Pfizer Investigational Site South Bend, Indiana, United States, 46601 United States, Massachusetts Pfizer Investigational Site Milford, Massachusetts, United States, 01757 United States, Missouri Pfizer Investigational Site Chesterfield, Missouri, United States, 63017 Pfizer Investigational Site Springfield, Missouri, United States, 65804 United States, North Carolina Pfizer Investigational Site Greensboro, North Carolina, United States, 27403 United States, Ohio Pfizer Investigational Site Cincinnati, Ohio, United States, 45219 United States, Oregon Pfizer Investigational Site Eugene, Oregon, United States, 97401 United States, Texas Pfizer Investigational Site San Antonio, Texas, United States, 78229 United States, Virginia Pfizer Investigational Site Alexandria, Virginia, United States, 22304 收起 <<
NCT00250458	-		Completed	-	-
NCT00471952	Migraine With Aura ... 展开 >> Migraine Without Aura 收起 <<	Phase 3	Completed	-	United States, Illinois ... 展开 >> Diamond Headache Clinic Chicago, Illinois, United States, 60614 收起 <<
NCT00897949	Migraine Headache	Phase 3	Completed	-	-
NCT00894556	-		Completed	-	-
NCT00897949	-		Completed	-	-
NCT00300924	Migraine	Phase 3	Completed	-	United States, California ... 展开 >> SanFrancisco Headache Clinic San Francisco, California, United States, 94109 United States, Illinois Diamond Headache Clinic Chicago, Illinois, United States, 60614 United States, Michigan Westside Family Medical Center Kalamazoo, Michigan, United States, 49009 United States, Missouri Clinvest Springfield, Missouri, United States Mercy Health Research St. Louis, Missouri, United States, 63141 United States, New York Elkind Headache Center Mount Vernon, New York, United States, 10550 United States, Ohio ClinExcel West Chester, Ohio, United States, 44121 收起 <<
NCT00899379	Migraine Headache	Phase 3	Completed	-	-
NCT00899379	-		Completed	-	-
NCT00360282	Migraine	Not Applicable	Completed	-	United States, Pennsylvania ... 展开 >> University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 收起 <<
NCT00898677	Migraine Headache	Phase 3	Completed	-	-
NCT00111709	Migraine	Phase 3	Completed	-	-
NCT00604812	Migraine Disorders	Phase 1	Completed	-	-
NCT00604812	-		Completed	-	-
NCT00898677	-		Completed	-	-
NCT00516737	Migraine	Phase 3	Completed	-	-
NCT00516737	-		Completed	-	-
NCT00897104	-		Completed	-	-
NCT01001234	Migraine, Acute	Phase 3	Completed	-	-
NCT00897104	Migraine Headache	Phase 3	Completed	-	-
NCT00812006	Migraine	Phase 3	Completed	-	-
NCT00894556	Acute Migraine	Phase 3	Completed	-	-
NCT01001234	-		Completed	-	-
NCT00397254	Migraine	Phase 4	Completed	-	United States, California ... 展开 >> Brian Koffman, MD Diamond Bar, California, United States, 91765 San Francisco Clinical Research Center San Francisco, California, United States, 94109 United States, Florida Physician Associates Oviedo, Florida, United States, 32765 United States, Georgia Dr. B. Abraham, PC Snellville, Georgia, United States, 33039 United States, Maryland Dhiren Shah, MD Prince Frederick, Maryland, United States, 20678 United States, Michigan Westside Family Medical Center Kalamazoo, Michigan, United States, 49009 United States, Missouri Clinvest Springfield, Missouri, United States, 65807 Mercy Health Research / Ryan Headache Center St. Louis, Missouri, United States, 63141 United States, North Carolina PharmQuest Greensboro, North Carolina, United States, 27401 United States, Pennsylvania Thomas Jefferson University Hospital Jefferson Headache Center Philadelphia, Pennsylvania, United States, 19107 收起 <<
NCT00719134	Episodic Migraine	Phase 4	Completed	-	United States, Massachusetts ... 展开 >> Pain Clinic at Beth Israel Deaconess Medical Center Brookline, Massachusetts, United States, 02445 收起 <<
NCT00397254	-		Completed	-	-
NCT00812006	-		Completed	-	-
NCT00753311	Migraine	Phase 4	Completed	-	Italy ... 展开 >> IRCCS San Raffaele Pisana, Clinical Trial Center Rome, Italy, I-00163 收起 <<
NCT01286207	Migraine Disorders	Phase 3	Completed	-	-
NCT01057160	Migraine	Phase 4	Completed	-	Germany ... 展开 >> Department of Neurology, University Hospital Essen Essen, Germany, 45147 收起 <<
NCT01004263	Acute Migraine With or Without... 展开 >> Aura in Adolescents 收起 <<	Phase 3	Completed	-	-
NCT01004263	-		Completed	-	-
NCT01306266	Chronic Post-traumatic Headach... 展开 >>e 收起 <<	Not Applicable	Withdrawn	August 2011	United States, Washington ... 展开 >> Madigan Army Medical Center - Neurology Clinic Tacoma, Washington, United States, 98431 收起 <<
NCT00719134	-		Completed	-	-
NCT02447991	Vestibular Migraine ... 展开 >> Migrainous Vertigo 收起 <<	Phase 2 Phase 3	Recruiting	June 2019	United States, California ... 展开 >> University of California, Los Angeles Recruiting Los Angeles, California, United States, 90095 Contact: Roxana G. Gonzalez 310-206-8511 GRGonzalez@mednet.ucla.edu Contact: Robert W. Baloh, M.D. 310-206-8511 rwbaloh@ucla.edu Principal Investigator: Robert W. Baloh, M.D. United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Deanna R Hofschulte 507-255-2972 hofschulte.deanna@mayo.edu United States, New York ICAHN School of Medicine at Mount Sinai Recruiting New York, New York, United States, 10029 Contact: Joanna Jen, MD Contact: Roxana Gonzalez 310-206-8511 grgonzalez@mednet.ucla.edu 收起 <<
NCT01286207	-		Completed	-	-

Rizatriptan {[allProObj[0].p_purity_real_show]}

Rizatriptan 纯度/质量文件产品仅供科研

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Rizatriptan 生物活性

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Rizatriptan 参考文献

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Rizatriptan {[allProObj[0].p_purity_real_show]}

Rizatriptan 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Rizatriptan 质控信息

Rizatriptan 生物活性

Rizatriptan 临床研究

Rizatriptan 参考文献

Rizatriptan 实验方案

Rizatriptan 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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Rizatriptan 纯度/质量文件产品仅供科研