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Felodipine is an inhibitor of L-type calcium channels.1 It induces relaxation of precontracted isolated porcine coronary artery segments (EC50 = 0.15 nM), which highly express L-type calcium channels.2 Felodipine is selective for L-type calcium channels over N-, R-, and P/Q-type channels at 10 µM, as well as the T-type Cav3.2 channel (IC50 = 6.8 µM).1,3 Felodipine preferentially inhibits L-type calcium channels in isolated rat portal vein over rat left ventricle (IC50s = 33.9 and 3,981 nM, respectively).4 It decreases mean arterial blood pressure and total peripheral resistance in a rabbit model of hypertension induced by renal artery ligation when administered intravenously at doses of 30 and 100 nmol/kg.5
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1. Selectivities of dihydropyridine derivatives in blocking Ca2+ channel subtypes expressed in Xenopus oocytes. J. Pharmacol. Exp. Ther. 291(2), 464-473 (1999).
2. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J. Pharmacol. Exp. Ther. 226(2), 330-334 (1983).
3. Molecular pharmacology of human Cav3.2 T-
4. Vascular selectivity of felodipine: Experimental pharmacology. J. Cardiovasc. Pharmacol. 15(Suppl 4), S11-S16 (1990).
5. Acute systemic and regional hemodynamic effects of felodipine, a new calcium antagonist, in conscious renal hypertensive rabbits. J. Cardiovasc. Pharmacol. 6(4), 707-712 (1984).