Amlodipine maleate is a dihydropyridine calcium channel blocker that serves as an orally active antianginal agent. It functions by blocking voltage-dependent L-type calcium channels, effectively inhibiting the initial influx of calcium ions. This drug is utilized in research focused on high blood pressure and cancer[1].[2].[3].
体内研究
In vivo, Amlodipine maleate administered at 5 mg/kg/day subcutaneously for two weeks significantly reduces systolic blood pressure in vascular smooth muscle cell ATP2B1 knockout (VSMC ATP2B1 KO) mice, showcasing its efficacy in managing hypertension[4].
Furthermore, at a dosage of 10 mg/kg administered intraperitoneally once daily for 20 days, it significantly retards tumor growth and prolongs the survival of mice bearing A431 tumors, reflecting its potential anti-cancer benefits[3].
体外研究
In cellular studies involving A431 cells, Amlodipine maleate at concentrations of 20 to 40 μM over 48 hours reduces BrdU incorporation—a marker for DNA synthesis—to 68.6% at 20 μM and to 26.3% at 30 μM, indicating its effect on cell proliferation[3].
Additionally, when pretreated for 1 hour at a concentration of 30 μM, it significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases in intracellular calcium levels in these cells[3].
Amlodipine maleate also inhibits the store-operated calcium influx triggered by Thapsigargin in Fluo-3-loaded cells at a concentration of 30 μM, demonstrating its ability to interfere with calcium signaling mechanisms[3].
搜索
