Olmesartan

Names

[ Name ]:
Olmesartan

[Synonym ]:
4-(2-Hydroxy-2-propanyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-1H-imidazole-5-carboxylic acid
Olmesartan Acid
MFCD00914967
Olmesartan
5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-

Biological Activity

[Description]:

Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

Research Areas >> Cardiovascular Disease

[In Vivo]

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].

[Animal admin]

Seven week-old male spontaneously hypertensive rats (SHR) are divided into five groups and fed a high fat diet (HFD) (60% kcal as fat) ad libitum. SHR are treated with vehicle (1% tragacanth gum solution), telmisartan (1 mg/kg), telmisartan (2 mg/kg), olmesartan (1 mg/kg) or olmesartan (2 mg/kg) once daily by gastric gavage. After more than 4 weeks-treatment, mean arterial blood pressure is measured for 24 h under a conscious state.

[References]

[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]. Komiya H, et al. Sleep/wakefulness behaviors in mice during pregnancy and pregnancy-associated hypertensive mice. Sleep. 2018 Mar 1;41(3).

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
738.3±70.0 °C at 760 mmHg

[ Melting Point ]:
186-188ºC

[ Molecular Formula ]:
C₂₄H₂₆N₆O₃

[ Molecular Weight ]:
446.502

[ Flash Point ]:
400.3±35.7 °C

[ Exact Mass ]:
446.206635

[ PSA ]:
129.81000

[ LogP ]:
3.72

[ Vapour Pressure ]:
0.0±2.6 mmHg at 25°C

[ Index of Refraction ]:
1.671

[ Storage condition ]:
-20°C Freezer

Safety Information

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
NI4014100

[ HS Code ]:
2921590090

Customs

[ HS Code ]: 2921590090

[ Summary ]:
2921590090. other aromatic polyamines and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

Articles

Structure-response relationship in electrospray ionization-mass spectrometry of sartans by artificial neural networks.

J. Chromatogr. A. 1438 , 123-32, (2016)

Quantitative structure-property relationship (QSPR) methods are based on the hypothesis that changes in the molecular structure are reflected in changes in the observed property of the molecule. Artif...

Synergistic, cytotoxic and apoptotic activities of olmesartan with NF-κB inhibitor against HeLa human cell line.

Toxicol. Mech. Methods 25 , 614-21, (2015)

Over expression of renin-angiotensin system (RAS) and nuclear factor-kappaB (NF-κB) has a major role in many cancers. It has been suggested that some angiotensin receptor blockers (ARBs) could reduce ...

Linear mixed-effects model of QTc prolongation for olmesartan medoxomil.

J. Clin. Pharmacol. , doi:10.1002/jcph.572, (2015)

Related Compounds

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