Fantofarone

Fantofarone is a calcium channel inhibitor.¹ It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC₅₀ = 0.61 nM) over α₁- and β-adrenergic, muscarinic, and histamine H₂ receptors in rat heart homogenates (IC₅₀s = >10, 4, >10, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT₁ and 5-HT₂, as well as histamine H₁ and adenosine A₁ receptors, in rat brain homogenates (IC₅₀s = >10, >10, 4, and >10 µM, respectively). Fantofarone inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC₅₀s = 1.4 and 150 nM, respectively).² It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC₅₀s = 5.64 and 96 nM, respectively).¹ It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM.³ Fantofarone prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis when administered at a dose of 50 µg/kg.⁴

WARNING This product is not for human or veterinary use.

1. Nokin, P., Clinet, M., Polster, P., et al. SR 33557, a novel calcium-antagonist: Interaction with [³H]-(±)-nitrendipine and [³H]-(−)-desmethoxy-verapamil binding sites in cerebral membranes. Naunyn Schmiedebergs Arch. Pharmacol. 339(1-2), 31-36 (1989).

2. Romey, G., Bois, P., and Lazdunski, M. Effects of two chemically related new Ca²⁺ channel antagonists, SR33557 (fantofarone) and SR33805, on the L-type cardiac channel. Eur. J. Pharmacol. 263(1-2), 101-105 (1994).

3. Manning, A., Mouton, J., and Chatelain, P. Fantofarone (SR 33557): Effect on post-ischaemic functional recovery in perfused rat hearts. Eur. J. Pharmacol. 220(2-3), 249-258 (1992).

4. Dongay, B., Dol-Gleizes, F., and Herbert, J.M. Effect of fantofarone, a new Ca²⁺ channel antagonist, on angioplasty-induced vasospasm in an atherosclerotic rabbit model. Biochem. Pharmacol. 55(12), 2047-2050 (1998).