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/非洛地平 细胞实验
Cell Line
Concentration
Treated Time
Description
References
IPSC-derived human neurons
100 nM
5 days
Felodipine reduced levels of A53T α-synuclein.
Nat Commun. 2019 Apr 18;10(1):1817.
MRSE (ATCC 35984)
8 μg/mL
24 hours
Evaluate the antibacterial effect of felodipine on MRSE, results showed that felodipine could effectively inhibit the growth of MRSE.
Bioact Mater. 2021 Nov 24;14:272-289.
MRSA (ATCC 43300)
8 μg/mL
24 hours
Evaluate the antibacterial effect of felodipine on MRSA, results showed that felodipine could effectively inhibit the growth of MRSA.
Bioact Mater. 2021 Nov 24;14:272-289.
Brain tissue
1.0 nM
30 minutes
Measure the effect of Felodipine on [3H]-isradipine binding in brain tissue. Results showed that Felodipine significantly inhibited [3H]-isradipine binding.
Br J Pharmacol. 1994 Aug;112(4):1017-24.
LL29 cells
6 µM and above
48 hours
Inhibited TGF-β1-induced collagen production without affecting cell viability
Felodipine monotherapy decreased systolic blood pressure. The combination with ramipril was more effective than ramipril alone but not significantly better than felodipine monotherapy. The beneficial effect of felodipine monotherapy on left ventricular hypertrophy was less prominent than that of ramipril, but its cardioprotective effect was improved when combined with ramipril.
Br J Pharmacol. 1997 Jun;121(3):503-10
Mice
Ethanol dependence model
Intraperitoneal injection
10 mg/kg
Single dose
Evaluate the effect of Felodipine on the ethanol withdrawal syndrome. Results showed that Felodipine did not significantly alter the behavioral manifestations of ethanol withdrawal.
Br J Pharmacol. 1994 Aug;112(4):1017-24.
CD1 ICR mice
Skin and soft tissue infection model
Subcutaneous injection
20 mg/kg and 40 mg/kg
Every 24 hours for 7 days
Evaluate the antibacterial effect of felodipine in a murine skin and soft tissue infection model, results showed that high-dose felodipine significantly reduced fluorescence intensity and bacterial burden at the infection site.
Bioact Mater. 2021 Nov 24;14:272-289.
ICR mice
Bleomycin-induced pulmonary fibrosis model
Intratracheal administration
3.3 mg/kg
Once daily for 14 days
Prevented and treated bleomycin-induced pulmonary fibrosis, improved lung function and reduced collagen deposition
Sci Rep. 2017 Jun 13;7(1):3439.
Mice
B6HD (N171-82Q) mice
Intraperitoneal injections
5 mg/kg
Three times a week for 6 weeks
Felodipine improved motor performance and reduced huntingtin aggregate numbers in B6HD mice.
Nat Commun. 2019 Apr 18;10(1):1817.
Mice
P301S transgenic mice (PS19)
Intraperitoneal injection
5 mg/kg
Daily for 14 days
Felodipine significantly attenuated tau-mediated microglial activation and NLRP3 expression, and significantly reduced tau hyperphosphorylation at S202/Thr205 and Thr212/Ser214 residues by inhibiting JNK/P38 signaling.
Mol Brain. 2024 Sep 2;17(1):62
Wistar-Kyoto rats
Fructose-fed rat model
Intubation
5 mg/kg/day
Once daily for 6 weeks
Felodipine significantly attenuated the increased levels in serum IL-18 and cardiac IL-18 mRNA as well as coronary perivascular fibrosis in fructose-fed rats.
搜索
