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158930-17-7

中文名称 罗曲普坦琥珀酸盐
英文名称 Frova
CAS 158930-17-7
分子式 C18H25N3O6
MOL 文件 158930-17-7.mol
更新日期 2024/06/03 14:41:41
158930-17-7 结构式 158930-17-7 结构式

基本信息

中文别名
夫罗曲坦琥珀酸
罗曲普坦琥珀酸盐
夫罗曲坦琥珀酸盐
夫罗曲普坦琥珀酸盐水合物
英文别名
Frova
Migard
Miguard
Frovelan
Unii-D28J6W18hy
Frovatriptan succinate [usan]
Frovatriptan succinate hydrate
Frovatriptan Succinate Monohydrate
(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

物理化学性质

熔点150-153°C
储存条件-20°C冷冻
溶解度可溶于DMSO(轻微)、甲醇(轻微、加热)、水(轻微、加热)
形态粉末
颜色白色至米色
CAS 数据库158930-17-7

常见问题列表

生物活性
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-HT1B (pK50 为 8.2) 和 5-HT1D 受体激动剂,选择性是 5-HT1A,5-HT1F 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。
靶点

5-HT 1B Receptor

8.2 (pEC 50 )

5-HT 1D Receptor

体外研究

Cerebral vasodilatation and neurogenic inflammation are considered to be prime movers in the pathogenesis of migraine. Activation of 5-HT 1B reverses cerebral vasodilatation and activation of 5-HT 1D prevents neurogenic inflammation. Frovatriptan has a high affinity for 5-HT 1B and 5-HT 1D receptors and a moderate affinity for the 5-HT 1A and 5-HT 1F receptors subtypes. Frovatriptan has a moderate affinity for the 5-HT 7 receptors, an action associated with coronary artery relaxation in the dog.

体内研究

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.

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