Frovatriptan succinate hydrate|158930-17-7|-陌孚医药/Medlife

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Frovatriptan succinate hydrate

目录号: PL05543 纯度: ≥99%

CAS No. :158930-17-7

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中文名称	Frovatriptan succinate hydrate
中文别名	罗曲普坦琥珀酸盐;夫罗曲坦琥珀酸 USP标准品;琥珀酸夫罗曲坦;夫罗曲普坦琥珀酸盐水合物;夫罗曲坦琥珀酸;夫罗曲坦琥珀酸盐;琥珀酸夫罗曲坦一水合物
英文名称	Frovatriptan succinate hydrate
英文别名	Frovatriptan succinate [USAN];Frova;butanedioic acid,(6R)-6-(methylamino)-6,7,8,9-tetrahydro-5H-carbazole-3-carboxamide,hydrate;Frovatriptan;FROVATRIPTAN SUCCINATE MONOHYDRATE;(+)-(R)-2,3,4,9-Tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide butanedioate (1:1),monohydrate;(+)-(R)-5,6,7,8-Tetrahydro-6-(methylamino)carbazole-3-carboxamide succinate (1:1),monohydrate;(R)-(+)-6-carbamoyl-N-methyl-2,3,4,9-tetrahydro-1H-carbazol-3-aminium 3-carboxypropanoate monohydrate;1H-Carbazole-6-carboxamide,2,3,;Frovatriptan succinate hydrate;UNII-D28J6W18HY;Frovatriptan succinate;R-(+) 3-Methylamino-6-carboxamido-1,2,3,4-tetrahydrocarbazole monosuccinate monohydrate;Migard;Miguard;Frovelan;(3R)-2,3,4,9-Tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide Butanedioic Acid Monohydrate;1H-Carbazole-6-carboxamide, 2,3,4,9-tetrahydro-3-(methylamino)-, (R)-, butanedioate (1:1), monohydrate;(R)-Frovatriptan succinate hydrate;SB 209509 succinate hydrate;VML 251 succinate hydrate;Frovatriptan succinate monohydrate;Unii-D28J6W18hy;Frovatriptan succinate [usan];Frovatriptan Succinate Monohydrate
Cas No.	158930-17-7
分子式	C₁₈H₂₅N₃O₆
分子量	379.41
包装储存	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) 是一种强效，高亲和力，选择性和具有口服活性的 5-HT_1B (pK₅₀ 为 8.2) 和 5-HT_1D 受体激动剂，选择性是 5-HT_1A，5-HT_1F 和 5-HT₇ 的 10 倍以上，是其他 5-HT，多巴胺，组胺 H₁ 和 α1-肾上腺素受体的 1000 倍以上。Frovatriptan succinate hydrate 可用于偏头痛的研究。

生物活性

Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT 1B (pK 50 of 8.2) and 5-HT 1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT 1B and 5-HT 1D over 5-HT 1A , 5-HT 1F , and 5-HT 7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H 1 , and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research.

性状

Solid

IC50 & Target[1][2]

5-HT1B Receptor 8.2 (pEC50) 5-HT1D Receptor

体外研究(In Vitro)

Cerebral vasodilatation and neurogenic inflammation are considered to be prime movers in the pathogenesis of migraine. Activation of 5-HT1B reverses cerebral vasodilatation and activation of 5-HT1D prevents neurogenic inflammation. Frovatriptan has a high affinity for 5-HT1B and 5-HT1D receptors and a moderate affinity for the 5-HT1A and 5-HT1F receptors subtypes. Frovatriptan has a moderate affinity for the 5-HT7 receptors, an action associated with coronary artery relaxation in the dog. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Oral bioavailability of Frovatriptan is 22%-30% and is not affected by food. Although the maximum concentration in the plasma is achieved in 2-3 hours, 60%-70% of this is achieved in 1 hour. A steady state is achieved in 4-5 days. Plasma protein binding is low at 15%. The most unique feature is the relative terminal long half-life of about 26 hours. Frovatriptan is chiefly metabolized by CYP1A2 and is cleared by the kidney and liver making moderate failure of either organ not a limiting factor in treatment.
Frovatriptan (0.1, 0.2, and 0.3 mg/kg; a single bolus intraduodenal administration) treatment produces an increase in carotid vascular resistance, which is sustained for at least 5 hours in dogs. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Kelman L. Review of frovatriptan in the treatment of migraine. Neuropsychiatr Dis Treat. 2008 Feb;4(1):49-54.
[2]. Comer MB. Et al. Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan. Headache. 2002 Apr;42 Suppl 2:S47-53.

溶解度数据	In Vitro: DMSO : 100 mg/mL (263.57 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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