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奥美沙坦

奥美沙坦用途

Olmesartan 是血管紧张素II受体 (AT1R) 拮抗剂,常用于治疗高血压。

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奥美沙坦名称

[ CAS 号 ]:
144689-24-7

[ 中文名 ]:
奥美沙坦

[ 英文名 ]:
Olmesartan

[中文别名 ]:

奥美沙坦酸

[英文别名 ]:

Olmesartan Acid
MFCD00914967
Olmesartan

奥美沙坦生物活性

[ 描述 ]:

Olmesartan 是血管紧张素II受体 (AT1R) 拮抗剂,常用于治疗高血压。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管紧张素受体

研究领域 >> 心血管疾病

[体内研究]

反复给予奥美沙坦(1 mg/kg,2 mg/kg,po)剂量依赖性地降低SHR中的平均动脉血压(MAP),而在10周内对体重和食物摄入没有显着影响[1]。奥美沙坦(5 mg/kg/d,po)和Hyd治疗可使小鼠的收缩压降低至相同程度。奥美沙坦治疗通过超声心动图,心脏重量,心肌细胞的横截面积和基因表达来评估心脏肥大。奥美沙坦治疗逆转了Ren-Tg小鼠ACE2和Mas受体的基因表达减少,并抑制了NADPH氧化酶(Nox)4表达和活性氧的增强[2]。

[动物实验]

将7周龄雄性自发性高血压大鼠（SHR）分成5组，随意喂食高脂肪饮食（HFD）（60％kcal作为脂肪）。通过胃管饲法每天一次用载体（1％黄蓍胶溶液），替米沙坦（1mg / kg），替米沙坦（2mg / kg），奥美沙坦（1mg / kg）或奥美沙坦（2mg / kg）治疗SHR。治疗超过4周后，在意识状态下测量平均动脉血压24小时。

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

[相关活性小分子]

奥美沙坦物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
738.3±70.0 °C at 760 mmHg

[ 熔点 ]:
186-188ºC

[ 分子式 ]:
C₂₄H₂₆N₆O₃

[ 分子量 ]:
446.502

[ 闪点 ]:
400.3±35.7 °C

[ 精确质量 ]:
446.206635

[ PSA ]:
129.81000

[ LogP ]:
3.72

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±2.6 mmHg at 25°C

[ 折射率 ]:
1.671

[ 储存条件 ]:
-20°C Freezer

奥美沙坦安全信息

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
NI4014100

[ 海关编码 ]:
2921590090

奥美沙坦海关

[ 海关编码 ]: 2921590090

[ 中文概述 ]:
2921590090. 其他芳香多胺及衍生物及它们的盐. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ 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%

奥美沙坦文献

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)

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