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Frovatriptan succinate hydrate

Frovatriptan succinate hydrate (Frova) 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。

CAS号

158930-17-7

分子式

C18H25N3O6

主要靶点

5-HT Receptor

仅限科研使用

Cat No : CM10939

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Synonyms

Frova|夫罗曲坦琥珀酸盐水合物 |Frovelan

验证数据展示

  • CAS No.: 158930-17-7

    Frovatriptan succinate hydrate
    CAS#: 158930-17-7

产品信息

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.

CAS号 158930-17-7
分子式 C18H25N3O6
主要靶点 5-HT Receptor
主要通路 神经科学|G蛋白偶联受体
分子量 379.41
纯度 99.95%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Frova|夫罗曲坦琥珀酸盐水合物 |Frovelan

靶点活性

Human 5-HT7 Receptor:6.7 (pki)|5-HT1B Receptor:8.6 (pki)|5-HT1D Receptor:8.4 (pki)

体内活性

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].?

体外活性

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].

溶解度

DMSO:60 mg/ml (158.14 mM)

参考文献

1.Kelman L. Review of frovatriptan in the treatment of migraine. Neuropsychiatr Dis Treat. 2008 Feb;4(1):49-54. 2.Comer MB. Et al. Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan. Headache. 2002 Apr;42 Suppl 2:S47-53.

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