Nebivolol hydrochloride是一种β1-肾上腺素受体选择性抑制剂,IC50为0.8 nM。
产品描述
Nebivolol hydrochloride is a cardioselective ADRENERGIC BETA-1 RECEPTOR ANTAGONIST (beta-blocker) that functions as a VASODILATOR through the endothelial L-arginine/ NITRIC OXIDE system. It is used to manage HYPERTENSION and chronic HEART FAILURE in elderly patients.
体外活性
Nebivolol处理患心肌梗塞大鼠,少量降低平均血压.开始静脉注射Nebivolol 10分钟,然后再口服处理患有心肌梗塞的大鼠,可以降低心肌凋亡.
体内活性
Nebivolol可以降低冠状动脉平滑肌细胞(haCSMCs)及内皮细胞(haECs)增殖,这种作用存在浓度和时间依赖性。Nebivolol在制备兔肺膜时,作用于beta 1-肾上腺素受体位点具有高亲和性和高度选择性。Nebivolol处理haCSMCs7天,明显抑制细胞增殖(IC50:6.1 μM)。Nebivolol处理haCSMCs 48小时,细胞凋亡率23%,且降低S期细胞数量。
细胞实验
Cells are exposed to different concentrations of Nebivolol (10-7~10-5 M) for 1, 2, 4, 7 and 14 days. Cell proliferation is analyzed by bromodeoxyuridine (BrdU) incorporation, and cell apoptosis is detected by PI or annexin V staining.(Only for Reference)
Cas No.
152520-56-4
分子式
C22H26ClF2NO4
分子量
441.9
别名
盐酸奈必洛尔;Nebivolol HCl;R 065824 hydrochloride;R-65824
储存和溶解度
Ethanol:4.4 mg/mL (10 mM)
DMSO:44.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years