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Frovatriptan succinate

CAS No. : 158930-09-7

MCE 站：Frovatriptan succinate

产品活性：Frovatriptan succinate ((R)-Frovatriptan succinate) 是一种强效，高亲和力，选择性和具有口服活性的 5-HT_1B (pK₅₀ 为 8.2) 和 5-HT_1D 受体激动剂，选择性是 5-HT_1A，5-HT_1F 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 可用于偏头痛的研究。

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 (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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