Frovatriptan succinate hydrate

SKU: orb1309659

Description

Frovatriptan succinate hydrate is a selective 5-HT1B/1D and 5-HT7 receptor agonist used in migraine research. It is effective against acute migraine attacks and associated symptoms, with studies supporting its use for menstrual migraine prophylaxis. Its pharmacological profile makes it a valuable tool for in vitro binding assays and in vivo models of trigeminovascular activation.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	158930-17-7
MW	379.41
Purity	99.95%
Formula	C₁₈H₂₅N₃O₆
SMILES	O.OC(=O)CCC(O)=O.CN[C@@H]1CCc2[nH]c3ccc(cc3c2C1)C(N)=O
Target	5-HT Receptor
Solubility	DMSO:60 mg/mL (158.14 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.27 mM)

Bioactivity

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Target IC50	5-HT7 receptor (human):6.7 (pki)\|5-HT1D receptor:8.4 (pki)\|5-HT1B receptor:8.6 (pki)
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. Read more...
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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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carotid, 5-HT1D Receptor, 5-HT1B Receptor, 5-HT1D, 5HT Receptor, 5-HT Receptor, 5-HT1B, 5-hydroxytryptamine Receptor, 5HTReceptor, 5-HT7, (R)-Frovatriptan succinate, Frova, Frovatriptan succinate, Frovatriptan succinate hydrate, Frovatriptan succinate Hydrate, Frovelan, Human 5-HT7 Receptor, menstrual, Inhibitor, nausea, migraine, orally, inhibit, SB 209509 succinate, Serotonin Receptor, phonophobia, photophobia, vascular, vomiting, VML 251 succinate

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Compound Identifiers

PubChem CID

152943 ↗

Key Properties

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No computed properties available.

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