中文名 | 琥珀酸福伐曲坦 |
英文名 | Frovatriptan Succinate |
别名 | 琥珀酸福伐曲坦 琥珀酸夫罗曲坦 夫罗曲普坦琥珀酸盐 化合物 T21407 琥珀酸福伐曲坦(琥珀酸夫罗曲坦) |
英文别名 | Vml 251 Sb-209509ax Fovatriptan succinate FrovatriptanSuccinate Frovatriptan Succinate (3R)-2,3,4,9-Tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide butanedioate |
CAS | 158930-09-7 |
化学式 | C18H23N3O5 |
分子量 | 361.4 |
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. |
上游原料 | 氰基硼氢化钠 苯甲醛 水合肼 甲醛 |