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Frovatriptan succinate hydrate

Catalog No. T11326   CAS 158930-17-7
Synonyms: Frovelan, Frova

Frovatriptan succinate hydrate (Frova) is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine. Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively.

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Frovatriptan succinate hydrate Chemical Structure
Frovatriptan succinate hydrate, CAS 158930-17-7
Pack Size Availability Price/USD Quantity
2 mg In stock $ 30.00
5 mg In stock $ 48.00
10 mg In stock $ 80.00
25 mg In stock $ 147.00
50 mg In stock $ 218.00
100 mg In stock $ 323.00
1 mL * 10 mM (in DMSO) In stock $ 54.00
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Purity: 99.95%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Frovatriptan succinate hydrate (Frova) is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine. Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively.
Targets&IC50 5-HT1D receptor:8.4 (pki), 5-HT7 receptor (human):6.7 (pki), 5-HT1B receptor:8.6 (pki)
In vitro 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. 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[1].
In vivo 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 has a low risk of interactions with other drugs.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[2].?
Synonyms Frovelan, Frova
Molecular Weight 379.41
Formula C18H25N3O6
CAS No. 158930-17-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/ml (158.14 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Anti-Parkinson's Disease Compound Library Orally Active Compound Library Bioactive Compounds Library Max Angiogenesis related Compound Library Antidepressant Compound Library Bioactive Compound Library Anti-Cancer Compound Library

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Keywords

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