Frovatriptan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、长效的 5-HT(1B/1D) 受体激动剂，可作为抗偏头痛化合物。

A potent, long lasting 5-HT(1B/1D) receptor agonist as a antimigraine agent.Migraine Appoved.

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. 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.

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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GPCR/G Protein

5-HT Receptor

5-HT Receptor

Neurological Disease

Migraine

158930-17-7

361.398

C18H23N3O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (263.57 mM)

CNC1CCC2=C(C1)C3=C(N2)C=CC(=C3)C(=O)N.C(CC(=O)O)C(=O)O.O

(R)-3-(methylamino)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamide succinate

(-20℃)

With Ice Pack

≥ 2 years