Lacidipine, a novel third-generation dihydropyridine calcium channel blocker used for hypertension. Lacidipine protects HKCs (human kidney cell) against apoptosis induced by ATP (adenosine triphosphate) depletion and recovery by regulating the caspase-3 pathway[3]. In addition to calcium channel-modulated vasodilation, lacidipine displays antioxidant activity greater than that of other dihydropyridine calcium antagonists. Lacidipine was effective in elderly patients (including those with isolated systolic hypertension), African Nigerian patients and patients with concurrent type 2 diabetes mellitus. Lower atherosclerotic progression and plaque formation with lacidipine compared with atenolol in patients completing the full 4 years of the study[4]. Lacidipine showed a significant reduction in elevated systolic blood pressure together with a great protection of ALT (alanine amine transferase) and SOD enzymes from the destructive effects of irradiation and hypertension in irradiated, hypertensive and lacidipine-treated rats[5]. Lacidipine-modified EPCs (Endothelial progenitor cells) via a partially CXCR4 (CXC chemokine receptor four) signaling contribute to enhanced endothelial repair capacity in hypertension[2]. In addition, lacidipine attenuates depression-like symptoms in reserpine-treated mice[6].
Lacidipine/拉西地平 细胞实验
Cell Line
Concentration
Treated Time
Description
References
guinea-pig ventricular myocytes
0.1 mM
2 minutes
To investigate the inhibitory effect of Lacidipine on L-type calcium current, results showed that 0.1 mM Lacidipine reduced L-type calcium current to 66±4% of control value within 2 minutes without altering the current-voltage relationship.
Br J Pharmacol. 1997 Feb;120(4):667-75
HEK293A cells
10 ×10−6, 20×10−6, and 40×10−6 Μ
6 hours
Inhibit IDO1/2 enzymatic activity
Adv Sci (Weinh). 2025 Jan;12(3):e2409310
MDA-MB-231 cells
10 ×10−6, 20×10−6, and 40×10−6 m
24 hours
Reduce the expression of IDO1, IDO2, and TDO2
Adv Sci (Weinh). 2025 Jan;12(3):e2409310
HeLa cells
5 ×10−6, 10×10−6, 20×10−6, 40×10−6, and 80×10−6 m
24 hours
Inhibit IFN γ-induced Kyn production
Adv Sci (Weinh). 2025 Jan;12(3):e2409310
murine aortic smooth muscle cells
30 μM
1-hour pretreatment followed by 4h and 24h
To investigate the effect of Lacidipine on ELDL-induced foam cell formation in smooth muscle cells. Results showed that Lacidipine significantly inhibited ELDL-mediated foam cell formation.
Assess cell viability and cell death, results showed lacidipine significantly reduced viability and induced cell death in OVCAR-5 cells
J Cheminform. 2024 Oct 7;16(1):112
ID8
10–40 μM
45 min
Measure oxygen consumption rate (OCR) and ATP production, results showed lacidipine significantly inhibited OCR and ATP production in ID8 cells in a dose-dependent manner
J Cheminform. 2024 Oct 7;16(1):112
Mouse peritoneal macrophages
1-20 μM
2-24 hours
To evaluate the inhibitory effect of Lacidipine on cholesterol esterification. Results showed that Lacidipine significantly inhibited cholesterol esterification at concentrations of 10 μM and 20 μM, reducing it to 30% and 24% of the control value, respectively.
Br J Pharmacol. 1997 Nov;122(6):1209-15
rat aortic smooth muscle cells
80pM-640pM
90 minutes
Investigation of Lacidipine's inhibitory effect on K+-induced contraction in rat aorta, with steady-state IC50 of 160pM
Br J Pharmacol. 1993 May;109(1):100-6
Lacidipine/拉西地平 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c mice
4T1-Luc breast cancer model
Oral
0.5 mg/kg, 1 mg/kg, 10 mg/kg, 20 mg/kg
Every 2 days for 21 days
Enhance the anti-tumor effect of chemotherapeutic agents
Adv Sci (Weinh). 2025 Jan;12(3):e2409310
New Zealand male rabbits
Hypercholesterolemic diet-induced atherosclerosis model
Oral
1, 3, 10 mg/kg/day
Once daily for two months
To evaluate the effect of Lacidipine on cholesterol esterification in the aortic arch. Results showed that Lacidipine reduced cholesterol esterification in a dose-dependent manner, with inhibition rates of 24%, 30%, and 41% at doses of 1, 3, and 10 mg/kg/day, respectively. Additionally, drug treatment reduced the total cholesterol content in the vessel wall.
Br J Pharmacol. 1997 Nov;122(6):1209-15
Rat
Rat aortic rings
In vitro organ bath
80pM-640pM
Single administration, monitored for up to 120 minutes
Evaluation of Lacidipine's inhibitory effect on vascular contraction under depolarizing conditions, showing slow and prolonged action
Br J Pharmacol. 1993 May;109(1):100-6
New Zealand White rabbits
Atherosclerotic model induced by cholesterol-rich diet
Oral (mixed with food)
1, 3, and 10 mg/kg/day
Once daily for 8 weeks
To investigate the effect of Lacidipine on atherosclerotic lesions induced by cholesterol-rich diet. Results showed that Lacidipine significantly reduced the extent of aortic fatty lesions (by 40%) at the dose of 10 mg kg-1 day-1 and dose-dependently inhibited carotid intimal hyperplasia (I/M ratios were 0.47±0.02, 0.40±0.09, and 0.32±0.02 for doses 1, 3, and 10 mg kg-1 day-1, respectively).
Once daily for 6 weeks (from 8 to 14 weeks of age)
Investigated the protective effects of Lacidipine on cardiac remodeling and renin production in salt-loaded SHRSP. The lowest dose (0.3 mg/kg) restored physiological downregulation of renin by high salt, reduced left ventricular hypertrophy, and decreased mRNA levels of atrial natriuretic factor and TGF-β1. Intermediate doses reduced blood pressure and PRA, but the highest dose (3 mg/kg) increased kidney renin mRNA.
Br J Pharmacol. 2001 Dec;134(7):1516-22
Stroke-prone spontaneously hypertensive rats (SHRSP) and Wistar Kyoto rats (WKY)
Salt-loaded stroke-prone spontaneously hypertensive rats (SL-SHRSP) and control (NS-SHRSP)
Oral
0.3 mg/kg/day and 1 mg/kg/day
Once daily for 6 weeks
To investigate the effect of lacidipine on cardiac hypertrophy and endothelin-1 (ET-1) gene expression. The results showed that lacidipine dose-dependently inhibited ventricle hypertrophy and ET-1 gene overexpression in SL-SHRSP, and this effect was unrelated to changes in systolic blood pressure (SBP).
Br J Pharmacol. 1996 Jun;118(3):659-64
Beagle dogs
Healthy beagle dogs
Oral
4 mg
Single dose
To evaluate the bioequivalence of three lacidipine formulations in beagle dogs. Results showed that the Cmax and AUC of the three formulations did not meet the bioequivalence criteria in 6 beagle dogs, but achieved bioequivalence in virtual simulations with 24 beagle dogs.
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