| Identification | Back Directory | [Name]
Amlodipine mesylate | [CAS]
246852-12-0 | [Synonyms]
Amlodipine mesylate USP/EP/BP
3-Ethyl 5-methyl 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-di
3-Ethyl 5-methyl 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate methanesulfonate
3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate,methanesulfonic acid | [Molecular Formula]
C20H25ClN2O5.CH4O3S | [MDL Number]
MFCD02682959 | [MOL File]
246852-12-0.mol |
| Hazard Information | Back Directory | [Uses]
Amlodipine mesylate, 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 mesylate can be used for the research of high blood pressure and cancer[1][2][3]. | [in vivo]
Amlodipine mesylate (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
Amlodipine mesylate (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: | ATP2B1loxP/loxP mice[4] | | Dosage: | 5 mg/kg/day | | Administration: | Subcutaneously implanted osmotic pump for 2 weeks | | Result: | Significantly decreased the blood pressure. |
| [IC 50]
L-type calcium channel | [References]
[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. DOI:10.2165/00003495-199550030-00009
[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. DOI:10.1016/j.ejphar.2004.04.006
[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. DOI:10.1038/hr.2017.92 |
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