| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
5-HT1B Receptor:8.2 (pEC50); 5-HT1D Receptor
Frovatriptan succinate hydrate primarily targets serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D. It has Ki values of 2.51 nM for 5-HT1B and 3.98 nM for 5-HT1D. The compound also shows moderate affinity for 5-HT7 (pKi = 6.7). It exhibits >1000-fold selectivity over other 5-HT receptors, dopamine, histamine H1, and α1-adrenoceptors. Activation of 5-HT1B/1D receptors leads to vasoconstriction of cranial blood vessels and inhibition of trigeminal nerve activation, which are key mechanisms for migraine relief. |
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| ln Vitro |
Migraine pathophysiology is thought to be primarily driven by neurogenic inflammation and cerebral vasodilatation. Brain vasodilatation is reversed by 5-HT1B activation, while neurogenic inflammation is avoided by 5-HT1D activation. 5-HT1B and 5-HT1D receptors are highly affinified for frovatriptan, whereas 5-HT1A and 5-HT1F receptor subtypes are only moderately affinized for the drug. Dog coronary artery relaxation is linked to frovatriptan's modest affinity for 5-HT7 receptors[1].
In vitro, Frovatriptan succinate hydrate acts as a potent agonist at 5-HT1B (pK50 = 8.2) and 5-HT1D receptors. It has pKi values of 8.6 for 5-HT1B and 8.4 for 5-HT1D. The compound is also a moderately potent 5-HT7 receptor agonist (pKi = 6.7). Its activity is measured in receptor binding and functional assays. The compound shows high selectivity for 5-HT1B/1D over other receptors. |
| ln Vivo |
Frovatriptan has an oral bioavailability of 22%–30%, which is unaffected by meals. 60%–70% of the plasma's maximal concentration is reached in an hour, even though it takes two to three hours to reach its maximum. It takes four to five days to reach a stable condition. The binding of plasma proteins is just 15%. The relative terminal long half-life of roughly 26 hours is the most distinctive trait. Since frovatriptan is mostly metabolized by CYP1A2 and excreted by the kidney and liver, mild failure of either organ should not be a treatment-limiting factor[1]. When dogs are treated with frovatriptan (0.1, 0.2, and 0.3 mg/kg; administered as a single bolus intraduodenal injection), their carotid vascular resistance increases and remains elevated for at least five hours[2].
In vivo, Frovatriptan succinate hydrate is orally active and clinically used for the acute treatment of migraine with or without aura. Its mechanism involves vasoconstriction of cranial blood vessels and inhibition of trigeminal nerve activation. The compound has been studied in animal models of migraine. Its long half-life and favorable pharmacokinetic profile make it effective for migraine treatment. Clinical studies have demonstrated its efficacy and safety. |
| Enzyme Assay |
The cell-free assay for Frovatriptan succinate hydrate involves evaluating its binding affinity to serotonin receptors. Radioligand binding assays are performed using membrane preparations from cells expressing recombinant human 5-HT1B, 5-HT1D, and 5-HT7 receptors. The compound is incubated with membranes and radiolabeled ligands. Competition binding experiments determine Ki or pKi values. Selectivity is assessed by testing against a panel of receptors.
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| Cell Assay |
For in vitro cellular assays, Frovatriptan succinate hydrate is typically dissolved in DMSO and diluted in cell culture medium. Cells expressing 5-HT1B, 5-HT1D, or 5-HT7 receptors are treated with various concentrations of the compound. Functional assays such as cAMP accumulation or calcium flux measurements are used to assess agonist activity. Potency (pEC50) and efficacy are determined from dose-response curves. Selectivity is confirmed by testing across multiple receptor subtypes.
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| Animal Protocol |
In vivo animal studies for Frovatriptan succinate hydrate are conducted in models of migraine and pain. The compound is administered orally or via other routes. Pain responses are measured using behavioral assays. Cranial blood vessel diameter is assessed. Pharmacokinetic parameters are determined from plasma samples. Efficacy is evaluated by comparing responses to untreated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Frovatriptan succinate hydrate include a molecular weight of 379.41 g/mol and molecular formula C18H25N3O6. The compound is orally active with good bioavailability. It has a long half-life compared to other triptans, which contributes to its sustained efficacy. The compound is typically stored at appropriate conditions as a research reagent. Detailed ADME parameters are available from clinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of Frovatriptan succinate hydrate has been well-characterized through clinical trials and post-marketing surveillance. Common side effects include dizziness, fatigue, and nausea. Serious adverse events are rare but may include cardiovascular events. The compound is contraindicated in patients with cardiovascular disease. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
See also: Frovatriptan (comment moved to); Frovatriptan Succinate (comment moved to).
Frovatriptan succinate hydrate is a potent, selective, and orally active 5-HT1B/1D receptor agonist (pKi = 8.6 and 8.4, respectively) and moderately potent 5-HT7 agonist (pKi = 6.7). It is clinically used for the acute treatment of migraine with or without aura. The compound shows >1000-fold selectivity over other receptors. Frovatriptan succinate hydrate is an approved antimigraine agent with a well-established safety and efficacy profile. |
| Molecular Formula |
C18H25N3O6
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|---|---|
| Molecular Weight |
379.40800
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| Exact Mass |
379.174
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| CAS # |
158930-17-7
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| Related CAS # |
Frovatriptan;158747-02-5;Frovatriptan succinate;158930-09-7
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| PubChem CID |
152943
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| Appearance |
White to off-white solid powder
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| Density |
1.27g/cm3
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| Boiling Point |
515.2ºC at 760mmHg
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| Flash Point |
265.4ºC
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| LogP |
2.306
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
426
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN[C@@H]1CCC2=C(C1)C3=C(N2)C=CC(=C3)C(=O)N.C(CC(=O)O)C(=O)O.O
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| InChi Key |
CUETXFMONOSVJA-KLQYNRQASA-N
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| InChi Code |
InChI=1S/C14H17N3O.C4H6O4.H2O/c1-16-9-3-5-13-11(7-9)10-6-8(14(15)18)2-4-12(10)17-13;5-3(6)1-2-4(7)8;/h2,4,6,9,16-17H,3,5,7H2,1H3,(H2,15,18);1-2H2,(H,5,6)(H,7,8);1H2/t9-;;/m1../s1
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| Chemical Name |
butanedioic acid;(6R)-6-(methylamino)-6,7,8,9-tetrahydro-5H-carbazole-3-carboxamide;hydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~263.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6357 mL | 13.1784 mL | 26.3567 mL | |
| 5 mM | 0.5271 mL | 2.6357 mL | 5.2713 mL | |
| 10 mM | 0.2636 mL | 1.3178 mL | 2.6357 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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