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概述
β1-肾上腺素受体拮抗剂(β1-adrenoceptor antagonist)。
Information
Metoprolol Tartrate (CGP 2175E) is a selectiveβ1 receptorblocker medication, used to treat hypertension and heart failure.
In vitro
Metoprolol, attenuates cardiomyocyte apoptosis in left ventricular (LV) myocardium of dogs with heart failure (HF). Metoprolol induces the expression of Bcl-2 independent of heart failure (HF) and that this independently confers protection.
In vivo
Metoprolol partly reverses the depressed left ventricular (LV) systolic pressure, positive and negative rates of changes in pressure development, ejection fraction, fractional shortening and cardiac output, as well as increased LV end-diastolic pressure in 20 weeks myocardial infarction (MI) rats. Metoprolol partially reverses the elevated levels of plasma norepinephrine and dopamine without affecting the elevated levels of epinephrine. Metoprolol treatment attenuates the development of cardiac dysfunction in streptozotocin (STZ)-diabetic rats. Metoprolol leads to reduced rates of palmitate oxidation, stimulation of glucose oxidation, and increases tissue ATP levels. Metoprolol leads to decreased maximum activity and decreased sensitivity of carnitine palmitoyltransferase I to malonyl-CoA. Metoprolol also increases sarco(endo) plasmic reticulum Ca(2+)-ATPase expression and prevents the reexpression of atrial natriuretic peptide in diabetic hearts of in streptozotocin (STZ)-diabetic rats. Metoprolol, attenuates the increase in collagen content in noninfarcted regions and prevents the increase in right ventricular weight/body weight, and its effect is similar to captopril in rat model with myocardial infarction (MI). Metoprolol treatment tends to increase right ventricular weight and heart weight.
Cell Data
cell lines：SU-DHL-1 and SU-DHL-9 cells
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
CGP 2175E
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Metoprolol Tartrate
生化机理
酒石酸美托洛尔（CGP 2175E）是一种选择性β1受体阻滞剂药物，用于治疗高血压和心力衰竭。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
β-1肾上腺素能受体拮抗剂
名称和识别符
EC号
260-148-9
分子类型
小分子
Isomeric SMILES
CC(C)NCC(COC1=CC=C(C=C1)CCOC)O.CC(C)NCC(COC1=CC=C(C=C1)CCOC)O.C(C(C(=O)O)O)(C(=O)O)O
分子量
684.81
Reaxy-Rn
6465966
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6465966&ln=
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 33 mg/mL (199.15 mM); Water: 33 mg/mL (199.15 mM); Ethanol: 33 mg/mL
安全和危险性（GHS）
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403: 存放在通风良好的地方。
P501: 将内容物/容器送到批准的废物处理厂处理
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
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