Felodipine

72509-76-3

C18H19Cl2NO4

DMSO : 100 mg/mL (260.25 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Membrane Transporter/Ion Channel; Autophagy; Neuronal Signaling

Felodipine is a long-acting 1, 4-dihydropyridine calcium channel blocker. Target: Calcium Channel Felodipine is a long-acting 1, 4-dihydropyridine calcium channel blocker (CCB)b. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ca.50 times more potent than nifedipine (IC50 of ca.8 nM) and ca.430 times than verapamil (IC50 of ca.65 nM) [1]. Felodipine significantly induces the transcription and secretion of IL-6 and IL-8 with ED50 values of 5.8 nM and 5.3 nM in primary human VSMC and lung fibroblasts, respectively, while propranolol or furosemide fails to affect the expression of the two IL genes [2]. Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM [3].