An agonist of 5-HT1B and 5-HT1D receptors
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Frovatriptan (succinate hydrate)

Item No. 23771

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
butanedioic acid, compd. with (R)-2,3,4,9-tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide, hydrate (1:1:1)
CAS Number
158930-17-7
Molecular Formula
C14H17N3O • C4H6O4 [H2O]
Formula Weight
379.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 10 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
245, 278 nm
SMILES
O=C(N)C1=CC2=C(NC3=C2C[C@H](NC)CC3)C=C1.OC(CCC(O)=O)=O.O
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
InChi Key
CUETXFMONOSVJA-KLQYNRQASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Frovatriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (Kis = 2.51 and 3.98 nM, respectively).1,2 It is selective for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2C, 5-HT3, and 5-HT7 receptors, as well as dopamine D1, D2, and D3, histamine H1, and α1-adrenergic receptors (Kis = >50 nM). Frovatriptan induces contractions in human basilar arteries isolated post-mortem, coronary arteries from transplant recipient hearts, and coronary arteries from donor hearts unsuitable for transplantation (EC50s = 13.8, 41.69, and 15.49 nM, respectively).3 It increases carotid vascular resistance in closed-chest and open-chest anesthetized dogs (ED50s = 6 and 1 nmol/kg, i.v., respectively).4 Formulations containing frovatriptan have been used in the treatment of migraines.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brown, A.M., Parsons, A.A., Raval, P., et al. SB 209509 (VML 251), a potent constrictor of rabbit basilar artery with high affinity and selectivity for human 5-HT1D receptors. Br. J. Pharmacol. 119(Suppl 1), 110P (1996).

    2. Comer, M.B. Pharmacology of the selective 5-HT1B/1D agonist frovatriptan. Headache 42(Suppl 2), S47-S53 (2002).

    3. Parsons, A.A., Raval, P., Smith, S., et al. Effects of the novel high-affinity 5-HT1B/1D-receptor ligand frovatriptan in human isolated basilar and coronary arteries. J. Cardiovasc. Pharmacol. 32(2), 220-224 (1998).

    4. Parsons, A.A., Parker, S.G., Raval, P., et al. Comparison of the cardiovascular effects of the novel 5-HT1B/1D receptor agonist, SB 209509 (VML251), and sumatriptan in dogs. J. Cardiovasc. Pharmacol. 30(1), 136-141 (1997).