1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Frovatriptan succinate hydrate

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

Cat. No.: HY-B1658A Purity: >99.0%
Handling Instructions

Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research.

For research use only. We do not sell to patients.

Frovatriptan succinate hydrate Chemical Structure

Frovatriptan succinate hydrate Chemical Structure

CAS No. : 158930-17-7

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10 mM * 1 mL in DMSO USD 396 In-stock
Estimated Time of Arrival: December 31
1 mg USD 95 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research[1][2].

IC50 & Target

5-HT1B Receptor

8.2 (pEC50)

5-HT1D Receptor

 

In Vitro

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[1].

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].

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

Clinical Trial
Molecular Weight

379.41

Formula

C₁₈H₂₅N₃O₆

CAS No.

158930-17-7

SMILES

O=C(O)CCC(O)=O.O=C(C1=CC2=C(NC3=C2C[[email protected]](NC)CC3)C=C1)N.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: >99.0%

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Keywords:

Frovatriptan succinate(R)-Frovatriptan succinateSB 209509 succinateVML 251 succinate5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1B5-HT1Dorallymigraine5-HT7carotidvascularmenstrualnauseavomitingphotophobiaphonophobiaInhibitorinhibitorinhibit

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Frovatriptan succinate hydrate
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