| Identification | Back Directory | [Name]
Frova | [CAS]
158930-17-7 | [Synonyms]
Frova
Migard
Miguard
Frovelan
Unii-D28J6W18hy
Frovatriptan succinate [usan]
Frovatriptan succinate hydrate
Frovatriptan Succinate Monohydrate
(3R)-2,3,4,9-Tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide Butanedioic Acid Monohydrate
1H-Carbazole-6-carboxamide, 2,3,4,9-tetrahydro-3-(methylamino)-, (R)-, butanedioate (1:1), monohydrate
Butanedioic acid, compd. with (R)-2,3,4,9-tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide (1:1), monohydrate | [Molecular Formula]
C18H25N3O6 | [MDL Number]
MFCD18251278 | [MOL File]
158930-17-7.mol |
| Chemical Properties | Back Directory | [Appearance]
White to Off-White Powder | [Melting point ]
150-153°C | [storage temp. ]
-20°C Freezer | [solubility ]
DMSO (Slightly), Methanol (Slightly, Heated), Water (Slightly, Heated) | [form ]
powder | [color ]
white to beige | [Water Solubility ]
H2O: 20mg/mL, clear | [CAS DataBase Reference]
158930-17-7 |
| Hazard Information | Back Directory | [Chemical Properties]
White to Off-White Powder | [Uses]
Serotonin 5-HT1B/1D receptor agonist. It is a triptan drug for the treatment of migraine headaches. Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head | [Brand name]
Frova (Endo). | [Biochem/physiol Actions]
Frovatriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. Frovatriptan has high affinity for the 5-HT(1B) and 5-HT(1D) receptors while affinity for 5-HT receptors other than 5-HT(1B/1D) is substantially lower with a pEC50 value of 8.2 for the 5-HT1B receptor, compared to a pEC50 value of 6.2 for the 5-HT7 receptor. | [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]. | [IC 50]
5-HT1B Receptor: 8.2 (pEC50); 5-HT1D Receptor | [storage]
Store at -20°C |
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J & K SCIENTIFIC LTD.
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