Frovatriptan succinate hydrate 是一种有效、高亲和力、选择性和口服活性的 5-HT1B、HT1D 受体激动剂和中等有效的 5-HT7 受体激动剂，pKi 值分别为 8.6、8.4 和 6.7。它可有效治疗各种偏头痛，包括恶心、呕吐、畏光和畏声等相关症状。

Frovatriptan succinate hydrate is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine. Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively.

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. 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[1].

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 has a low risk of interactions with other drugs.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[2].?

158930-17-7

C18H25N3O6

379.41

夫罗曲坦琥珀酸盐水合物 ;Frova;Frovelan

DMSO:60 mg/ml (158.14 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years