罗曲普坦琥珀酸盐
中文名称 | 罗曲普坦琥珀酸盐 |
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中文同义词 | 夫罗曲普坦琥珀酸盐水合物;罗曲普坦琥珀酸盐;夫罗曲坦琥珀酸;夫罗曲坦琥珀酸盐;夫罗曲坦琥珀酸盐水合物;琥珀酸夫罗曲坦一水合物 |
英文名称 | Frova |
英文同义词 | Frova;(3R)-2,3,4,9-Tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide Butanedioic Acid Monohydrate;Frovatriptan Succinate Monohydrate;Frovelan;Migard;Miguard;1H-Carbazole-6-carboxamide, 2,3,4,9-tetrahydro-3-(methylamino)-, (R)-, butanedioate (1:1), monohydrate;Butanedioic acid, compd. with (R)-2,3,4,9-tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide (1:1), monohydrate |
CAS号 | 158930-17-7 |
分子式 | C18H25N3O6 |
分子量 | 0 |
EINECS号 | |
相关类别 | Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals |
Mol文件 | 158930-17-7.mol |
结构式 |
罗曲普坦琥珀酸盐 性质
熔点 | 150-153°C |
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储存条件 | 2-8°C |
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 |
5-HT 1B Receptor 8.2 (pEC 50 ) |
5-HT 1D Receptor
|
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.
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.
安全信息
海关编码 | 2933995500 |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-B1658A | 罗曲普坦琥珀酸盐 Frovatriptan succinate hydrate | 158930-17-7 | 1mg | 304元 |
2024/08/19 | HY-B1658A | Frovatriptan succinate hydrate | 5 mg | 620元 |