Amlodipine是一种长效钙通道拮抗剂，通过阻断 L 型钙通道用于降低血压和预防胸痛，用于高血压和心绞痛的研究。
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Excepted Quantity
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Limited Quantity
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Amlodipine, a third-generation dihydropyridine calcium antagonist, has a mode of action and pharmacodynamic profile which are comparable to those of conventional compounds in this series, such as nifedipine[3]. Among combinations of hypertension medications, a β-blocker such as bisoprolol with a calcium channel blocker such as amlodipine is an effective combination therapy for hypertension, with distinct and complimentary modes of action[4]. Black triangle In the comparison with amlodipine monotherapy, >70% of olmesartan medoxomil/amlodipine recipients, some requiring upwards dosage adjustment, met BP goals. Peripheral oedema was significantly less common in olmesartan medoxomil/amlodipine 40 mg/10 mg per day than amlodipine monotherapy 10 mg/day recipients[5]. Maximal amlodipine concentrations in mothers ranged from 4.4 to 14.7 ng/mL in plasma, and 6.5 to 19.7 ng/mL in milk (Average milk/plasma ratio: 1.4). RID was 3.4% of the maternal weight-adjusted dose. All plasma concentrations in infants were under the quantitation limit (0.4 ng/mL). Infant exposure to amlodipine in breast milk appears very small, suggesting that amlodipine can be used with little influence on infants during breastfeeding[6].
Amlodipine/氨氯地平 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Ishikawa cells
10 μM, 15 μM
12 h
To evaluate the effect of AM on the apoptosis of Ishikawa cells, the results showed that AM induced cell apoptosis.
Cells. 2022 Oct 8;11(19):3156.
Ishikawa cells
15 μM
48 h
To evaluate the effect of AM on the proliferation of Ishikawa cells, the results showed that AM inhibited cell proliferation.
Cells. 2022 Oct 8;11(19):3156.
Ishikawa cells
0, 1.25, 5, 10, 12.5, 20, 25, 40, 50 μM
72 h
To evaluate the effect of AM on the proliferation of Ishikawa cells, the results showed that AM inhibited cell proliferation.
Cells. 2022 Oct 8;11(19):3156.
MGC803 cells
0, 5, 10, 20 µM
24, 48, 72 h
To evaluate the effect of amlodipine on cell proliferation, results showed that amlodipine inhibited GC cell proliferation in a dose-dependent manner.
Funct Integr Genomics. 2024 Apr 18;24(3):77.
HGC27 cells
0, 5, 10, 20 µM
24, 48, 72 h
To evaluate the effect of amlodipine on cell proliferation, results showed that amlodipine inhibited GC cell proliferation in a dose-dependent manner.
Funct Integr Genomics. 2024 Apr 18;24(3):77.
vascular smooth muscle cells (VSMCs)
5 μM
24 h
To investigate the effect of amlodipine on VSMC differentiation, results showed that amlodipine increased the expression of α-SMA, CNN1, and SM-MHC but decreased OPN expression.
Br J Pharmacol. 2019 Jul;176(13):2306-2320.
Amlodipine/氨氯地平 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
Subcutaneous transplanted tumor model
Peritoneal injection
15 mg/kg, 20 mg/kg
Every two days for 14 days
To evaluate the inhibitory effect of AM on tumor growth in vivo, the results showed that AM significantly inhibited tumor growth.
Cells. 2022 Oct 8;11(19):3156.
NKG mice
Subcutaneous xenograft model
Oral
10 mg/kg
Once daily for 28 days
To evaluate the effect of amlodipine on tumor growth in vivo, results showed that amlodipine significantly reduced tumor volume and weight in the SYT4-OE group.
Funct Integr Genomics. 2024 Apr 18;24(3):77.
Spontaneously hypertensive rats (SHRs)
Spontaneously hypertensive rat model
Oral
2 mg/kg
Once daily for 10 weeks
To investigate the effect of amlodipine on blood pressure and vascular function in SHRs, results showed that amlodipine promoted VSMC differentiation by upregulating miR-21 expression.
Br J Pharmacol. 2019 Jul;176(13):2306-2320.
Sprague-Dawley rats
Amlodipine-induced shock model
Intravenous injection
17 mg/kg
Three doses at 5, 30, and 60 minutes
To evaluate the efficacy of methylene blue in an amlodipine-induced shock model. Results showed that the methylene blue group had significantly higher survival time, heart rate, and mean arterial pressure compared to the control group.
Ann Emerg Med. 2015 Apr;65(4):410-5
Rats
High-fat diet-induced non-alcoholic fatty liver disease model
Intraperitoneal injection
5mg/kg
Twice a week for 12 weeks
Vitamin D supplementation alleviates high-fat diet-induced non-alcoholic fatty liver disease by modulating gut microbiota and metabolism.
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