Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker. Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ~50 times more potent than nifedipine (IC50 of ~8 nM) and ~430 times than verapamil (IC50 of ~65 nM) [3]. 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[4]. 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[5]. In hypertensive patients, felodipine does not appear to significantly affect glomerular filtration rate, creatinine clearance, glucose tolerance, or plasma lipoprotein concentrations. In the management of hypertension, felodipine 5-40 mg/d significantly reduces systolic and diastolic BP. Adverse effects associated with felodipine are similar to those of other dihydropyridine calcium-channel antagonists and include peripheral edema, headache, dizziness, flushing, and fatigue. Felodipine appears to be safe and effective for the management of hypertension when used alone or in combination with other antihypertensive agents[6].
Felodipine 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
H9C2 cells
Function assay
Inhibition of L-VDCC in rat H9C2 cells assessed as effect on calcium level by Fluo-4 fluorescence assay
19880323
HepG2 (DPX-2) cells
Function assay
24 h
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50=1.9 μM
20966043
HepG2 cells
Function assay
24 h
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50=23.4 μM
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