Frovatriptan succinate  (Synonyms: (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate)

Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT_1B (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT_1B and 5-HT_1D over 5-HT_1A, 5-HT_1F, and 5-HT₇ and >1000-fold selectivity over other 5-HT, dopamine, histamine H₁, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research^[1][2].

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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

361.39

C₁₈H₂₃N₃O₅

158930-09-7

夫罗曲坦琥珀酸盐

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kelman L. Review of frovatriptan in the treatment of migraine. Neuropsychiatr Dis Treat. 2008 Feb;4(1):49-54.  [Content Brief]

  [2]. Comer MB. Et al. Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan. Headache. 2002 Apr;42 Suppl 2:S47-53.  [Content Brief]