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Frovatriptan succinate hydrate

CAS No. : 158930-17-7

MCE 站：Frovatriptan succinate hydrate

产品活性：Frovatriptan succinate hydrate 是一种强效，高亲和力，选择性和口服活性的 5-HT_1B ，5-HT_1D 受体激动剂和中等强度的 5-HT₇ 受体激动剂，pK_i 值分别为 8.6、8.4 和 6.7。Frovatriptan succinate hydrate 可以有效治疗所有偏头痛，包括恶心，呕吐，畏光和畏音的相关症状。Frovatriptan succinate hydrate 也可用于短期预防经期偏头痛。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: 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-HT₇ receptors, an action associated with coronary artery relaxation in the dog.

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 has a low risk of interactions with other drugs.

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