|2-(5-((1H-1,2,4-三唑-1-基)甲基)-1H-吲哚-3-基)-N,N-二甲基乙胺苯甲酸盐|CsnPharm

CAS No.: 145202-66-0

Rizatriptan benzoate/苯甲酸利扎曲坦 Catalog No. CSN18707

Synonyms: MK 462;MK-462 Benzoate;Rizatriptan (benzoate salt)

Rizatriptan Benzoate is a triptan-class 5-HT1 receptor agonist, used to treat migraine headaches.

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技术信息

生物活性

描述Rizatriptan Benzoate is an orally active serotonin 5-HT(1) receptor agonist that potently and selectively binds to 5-HT(1B/1D) subtypes. Oral rizatriptan 5 and 10mg have shown greater efficacy than placebo in providing pain relief, an absence of pain, relief from associated symptoms, normal functional ability and an improvement in patient quality of life. Rizatriptan 10mg provides faster pain relief and a higher percentage of patients with an absence of pain and normal functional ability at 2 hours than naratriptan 2.5mg or zolmitriptan 2.5mg^[3]. Rizatriptan Benzoate is a selective 5-hydroxy tryptamine receptor agonist with anti migraine property. The rizatriptan benzoate oral disintegrating strip is potentially a useful tool for an effective treatment of migraine with improved bioavailability, rapid onset of action and with increased patient compliance^[4]. Rizatriptan benzoate significantly reduced expression of the mRNAs for proenkephalin and substance P. Rizatriptan benzoate may inhibit the analgesic effect of the endogenous pain modulatory system^[5]. In addition, the brain uptake potential of optimized RB-SLNs (rizatriptan benzoate-loaded solid lipid nanoparticles) to be 18.43-folds higher with respect to the pure drug in its free form, post 2 h of oral drug administration. RB-SLNs have distinctly improved brain target ability^[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
NCT01381497	-	-	Completed	-	-
NCT01435941	-	-	Completed	-	-
NCT00910689	Migraine Headache	Phase 4	Completed	-	United States, Ohio ... more >> Ohio University Athens, Ohio, United States, 45701 OrthoNeuro, Inc. Westerville, Ohio, United States, 43081 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5545 mL
- 12.7724 mL
- 25.5447 mL
- 5 mM
- 0.5109 mL
- 2.5545 mL
- 5.1089 mL
- 10 mM
- 0.2554 mL
- 1.2772 mL
- 2.5545 mL

技术信息

CAS号

145202-66-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H25N5O2

运输

蓝冰

分子量

391.47

别名

MK 462;MK-462 Benzoate;Rizatriptan (benzoate salt);Rizatriptan Benzoate;MK-0462;2-(5-((1H-1,2,4-TRIAZOL-1-YL)METHYL)-1H-INDOL-3-YL)-N,N-DIMETHYLETHANAMINE BENZOATE;Maxalt

溶解度

DMSO	80.0 mg/mL (204.4 mM) warming
Water	58.0 mg/mL (148.2 mM)

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01381497	-	-	Completed	-	-
NCT01435941	-	-	Completed	-	-
NCT00910689	Migraine Headache	Phase 4	Completed	-	United States, Ohio ... more >> Ohio University Athens, Ohio, United States, 45701 OrthoNeuro, Inc. Westerville, Ohio, United States, 43081 Collapse <<
NCT00910689	-	-	Completed	-	-
NCT00250458	Migraine	Phase 3	Completed	-	-
NCT01381523	-	-	Completed	-	-
NCT00250458	-	-	Completed	-	-
NCT01057160	Migraine	Phase 4	Completed	-	Germany ... more >> Department of Neurology, University Hospital Essen Essen, Germany, 45147 Collapse <<
NCT00360282	Migraine	Not Applicable	Completed	-	United States, Pennsylvania ... more >> University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 Collapse <<
NCT00360282	-	-	Completed	-	-
NCT00111722	Migraine	Phase 3	Completed	-	-
NCT00111709	Migraine	Phase 3	Completed	-	-
NCT00719134	Episodic Migraine	Phase 4	Completed	-	United States, Massachusetts ... more >> Pain Clinic at Beth Israel Deaconess Medical Center Brookline, Massachusetts, United States, 02445 Collapse <<
NCT02447991	Vestibular Migraine ... more >> Migrainous Vertigo Collapse <<	Phase 2 Phase 3	Recruiting	June 2019	United States, California ... more >> 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 Collapse <<
NCT00719134	-	-	Completed	-	-
NCT00397254	-	-	Completed	-	-
NCT00095004	Migraine	Phase 3	Completed	-	-
NCT00092963	Migraine	Phase 3	Completed	-	-
NCT00397254	Migraine	Phase 4	Completed	-	United States, California ... more >> 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 Collapse <<
NCT01001234	-	-	Completed	-	-
NCT00898677	Migraine Headache	Phase 3	Completed	-	-
NCT00898677	-	-	Completed	-	-
NCT00812006	-	-	Completed	-	-
NCT01286207	Migraine Disorders	Phase 3	Completed	-	-
NCT00812006	Migraine	Phase 3	Completed	-	-
NCT01306266	Chronic Post-traumatic Headach... more >>e Collapse <<	Not Applicable	Withdrawn	August 2011	United States, Washington ... more >> Madigan Army Medical Center - Neurology Clinic Tacoma, Washington, United States, 98431 Collapse <<
NCT01286207	-	-	Completed	-	-
NCT01001234	Migraine, Acute	Phase 3	Completed	-	-
NCT00899379	Migraine Headache	Phase 3	Completed	-	-
NCT00897949	Migraine Headache	Phase 3	Completed	-	-
NCT00604812	-	-	Completed	-	-
NCT00897949	-	-	Completed	-	-
NCT00604812	Migraine Disorders	Phase 1	Completed	-	-
NCT00899379	-	-	Completed	-	-
NCT00897104	Migraine Headache	Phase 3	Completed	-	-
NCT00897104	-	-	Completed	-	-
NCT00516737	Migraine	Phase 3	Completed	-	-
NCT01004263	Acute Migraine With or Without... more >> Aura in Adolescents Collapse <<	Phase 3	Completed	-	-
NCT01004263	-	-	Completed	-	-
NCT00516737	-	-	Completed	-	-
NCT00471952	Migraine With Aura ... more >> Migraine Without Aura Collapse <<	Phase 3	Completed	-	United States, Illinois ... more >> Diamond Headache Clinic Chicago, Illinois, United States, 60614 Collapse <<

Rizatriptan benzoate/苯甲酸利扎曲坦 Catalog No. CSN18707

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