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Referencia número: HY-B1658B

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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.

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No. CAS: 158930-09-7
Fòrmula: C₁₈H₂₃N₃O₅
Peso molecular:361.39

Almacenamiento:

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

Data Sheet (276 KB)

Frovatriptan succinate Chemical Structure

No. CAS: 158930-09-7

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Actividad biológica

Descripciòn

IC₅₀ & Target^[2]

5-HT_1A Receptor

5-HT_1B Receptor

5-HT_1F Receptor

5-HT₇ Receptor

5-HT_1B Receptor

8.2 (pEC₅₀)

5-HT_1D Receptor

Ver todos los productos específicos de isoformas 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^[1].

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

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^[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].

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

Chemical Information

No. CAS 158930-09-7
Peso molecular 361.39
Fòrmula C₁₈H₂₃N₃O₅
SMILES

O=C(O)CCC(O)=O.O=C(C1=CC2=C(NC3=C2C[C@H](NC)CC3)C=C1)N
Synonyms

(R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

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Frovatriptan succinate

Ver todos los productos específicos de isoformas 5-HT Receptor

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

Frovatriptan succinate Related Classifications

HY-B1658B Related Classifications