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Frovatriptan succinate hydrate

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

Print datasheet

Synonyms

Human 5-HT7 Receptor|inhibit|Frovatriptan succinate hydrate|Frovatriptan succinate Hydrate|Frovelan|Frova|Frovatriptan succinate|5-HT Receptor|5HT Receptor|5-HT1B|5-HT1B Receptor|5-HT1D|5-hydroxytryptamine Receptor|5HTReceptor|5-HT7|5-HT1D Receptor|(R)-Frovatriptan succinate|carotid|VML 251 succinate|vomiting|vascular|Serotonin Receptor|SB 209509 succinate|夫罗曲坦琥珀酸盐水合物?|Inhibitor|menstrual|migraine|nausea|orally|photophobia|phonophobia

验证数据展示

  • CAS No.: 158930-17-7

    Frovatriptan succinate hydrate
    CAS#: 158930-17-7

产品信息

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 | Shipping with blue ice.
别名 Human 5-HT7 Receptor|inhibit|Frovatriptan succinate hydrate|Frovatriptan succinate Hydrate|Frovelan|Frova|Frovatriptan succinate|5-HT Receptor|5HT Receptor|5-HT1B|5-HT1B Receptor|5-HT1D|5-hydroxytryptamine Receptor|5HTReceptor|5-HT7|5-HT1D Receptor|(R)-Frovatriptan succinate|carotid|VML 251 succinate|vomiting|vascular|Serotonin Receptor|SB 209509 succinate|夫罗曲坦琥珀酸盐水合物?|Inhibitor|menstrual|migraine|nausea|orally|photophobia|phonophobia

靶点活性

5-HT1B receptor:8.6 (pki)|5-HT7 receptor (human):6.7 (pki)|5-HT1D receptor:8.4 (pki)

体内活性

Frovatriptan主要通过CYP1A2代谢，并通过肾脏和肝脏清除，中度肾脏或肝脏功能衰竭并不是治疗的限制因素。Frovatriptan与其他化合物的相互作用风险较低。其口服生物利用度为22%-30%，不受食物影响。虽然最高血浆浓度在2-3小时内达到，但60%-70%的浓度在1小时内就可以达到。稳态在4-5天内实现。血浆蛋白结合率低，为15%。最独特的特点是其相对较长的末端半衰期，大约为26小时[2]。

体外活性

Frovatriptan 对5-HT1B和5-HT1D受体具有高亲和力，并对5-HT1A和5-HT1F受体亚型具有中等亲和力。Frovatriptan 对5-HT7受体也表现出中等亲和力，这一作用与犬类冠状动脉的松弛相关。5-HT1B受体的激活可逆转脑血管扩张，而5-HT1D受体的激活则可预防神经源性炎症[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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