Bioactivity | Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3]. | ||||||||||||
Invitro | Amlodipine (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].Amlodipine (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].Amlodipine (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3]. | ||||||||||||
In Vivo | Amlodipine (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].Amlodipine (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3]. Animal Model: | ||||||||||||
Name | Amlodipine | ||||||||||||
CAS | 88150-42-9 | ||||||||||||
Formula | C20H25ClN2O5 | ||||||||||||
Molar Mass | 408.88 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Kishen G. Bulsara, et al. Amlodipine. [2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586. [3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12. [4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87. |