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.
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 receptorsBr. J. Pharmacol.119(Suppl 1)110P(1996) 2.Comer, M.B.Pharmacology of the selective 5-HT1B/1D agonist frovatriptanHeadache42(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 arteriesJ. 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 dogsJ. Cardiovasc. Pharmacol.30(1)136-141(1997)