Frovatriptan (succinate hydrate)

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.

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).