An AT1 receptor antagonist and active metabolite of olmesartan medoxomil
Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure[1][2].
Olmesartan (0.7-5 mM; 24, 48 and 72?h) inhibits the growth of HeLa cells as a concentration- and time-dependent mode[3].
Repeated dosing of olmesartan (1 mg/kg, 2 mg/kg, p.o.) dose-dependently decreases mean arterial blood pressure (MAP) in SHR without significant influence on body weight and food intake during 10 weeks[1]. Olmesartan (5 mg/kg/d, p.o.) and Hyd treatments lower systolic blood pressure to the same degree in mice. Olmesartan treatment inhibits cardiac hypertrophy, evaluated by echocardiography, heart weight, cross-sectional area of cardiomyocytes, and gene expression. Olmesartan treatment reverses decreased gene expressions of ACE2 and Mas receptor of Ren-Tg mice and inhibits enhanced NADPH oxidase (Nox)4 expression and reactive oxygen species[2].
参考文献:
[1]. Yanagihara H, et al. Effects of telmisartan and olmesartan on insulin sensitivity and renal function in spontaneously hypertensive rats fed a high fat diet. J Pharmacol Sci. 2016 Jul;131(3):190-7.
[2]. Tanno T, et al. Olmesartan Inhibits Cardiac Hypertrophy in Mice Overexpressing Renin Independently of Blood Pressure: Its Beneficial Effects on ACE2/Ang(1-7)/Mas Axis and NADPH Oxidase Expression. J Cardiovasc Pharmacol. 2016 Jun;67(6):503-9.
[3]. Bakhtiari E, et al. Synergistic, cytotoxic and apoptotic activities of olmesartan with NF-κB inhibitor against HeLa human cell line. Toxicol Mech Methods. 2015;25(8):614-21.
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