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Nebivolol HCl

产品号 S1549 公司名称 Selleck Chemicals
CAS号 152520-56-4 公司网站 http://www.selleckchem.com
分子式 C22H26ClF2NO4 电 话 (877) 796-6397
分子量 441.8959464 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 72738

产品价格信息

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产品别名

标题
Nebivolol HCl
IUPAC标准名
(1R)-1-[(2R)-6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl]-2-{[(2R)-2-[(2S)-6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl]-2-hydroxyethyl]amino}ethan-1-ol hydrochloride
IUPAC传统名
dexnebivolol hydrochloride
别名
Bystolic
R-67145

产品登记号

CAS号 152520-56-4

产品性质

作用靶点 adrenergic receptor
成盐信息 HCL
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area
Description Cardiovascular Disease
Biological Activity
Description Nebivolol selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
Targets β1-adrenoceptor
IC50 0.8 nM [1]
In Vitro Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (Ki value = 0.9 nM and beta 2/beta 1 ratio = 50). [1] Nebivolol displays β1-adrenoceptor selectivity with the Ki(β2)/Ki(β1) value of 40.7 judged by competition experiments to 3H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, Kiβ2) or ICI 118.551 (50 nM, Kiβ1). [2] Nebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed. [3]
In Vivo Administratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly. [4]
Clinical Trials A Phase IV study of comparative effects of Nebivolol versus Metoprololon on fatigue and quality of life has been completed.
Features Nebivolol is highly cardioselective under certain circumstances.
Protocol
Cell Assay [3]
Cell Lines Human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs)
Concentrations Dissolved in 100% methanol and diluted with three volumes of growth medium to obtain a stock solution of 10-3 M, final concentration 10-7~10-5 M
Incubation Time 1, 2, 4, 7 and 14 days
Methods 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.
Animal Study [4]
Animal Models Male Sprague Dawley rat myocardial infarction (MI) model
Formulation Dissolved in DMSO and diluted in saline
Doses 2.0 mg/kg
Administration Gastric gavage once daily
References
[1] Pauwels PJ, et al. Mol Pharmacol, 1988, 34(6), 843-851.
[2] Brixius K, et al. Br J Pharmacol, 2001, 133(8), 1330-1338.
[3] Brehm BR, et al. Cardiovasc Res, 2001, 49(2), 430-439.
[4] Mercanoglu G, et al. Circ J, 2008, 72(4), 660-670.