| Name | Frovatriptan succinate hydrate |
| 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. |
| 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].? |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/ml (158.14 mM)
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| Keywords | Serotonin Receptor | 5-HT1D | 5-HT Receptor | Frovatriptan succinate hydrate | orally | Inhibitor | SB 209509 succinate | menstrual | Frovatriptan succinate | (R)-Frovatriptan succinate | inhibit | 5-HT7 | 5-hydroxytryptamine Receptor | vomiting | carotid | migraine | 5-HT1B | VML 251 succinate | photophobia | phonophobia | Frovatriptan succinate Hydrate | vascular | nausea |
| Inhibitors Related | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Parkinson's Disease Compound Library | Angiogenesis related Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Serotonin Receptor-Targeted Compound Library |
United States
