包装: | 1mg |
规格: | 98% |
市场价: | 2080元 |
分子量: | 445.9 |
Background:
(±)-Nebivolol-d4is intended for use as an internal standard for the quantification of nebivolol by GC- or LC-MS. Nebivolol is a potent and selective β1-adrenergic receptor (β1-AR) antagonist (IC50s = 7.41 and 251 nM for β1- and β2-ARs, respectively, in a radioligand binding assay using rabbit lung membrane preparations).1It is also selective for β1-ARs over serotonin 5-HT1Aand 5-HT2, α1- and α2-adrenergic, histamine H1, and dopamine D2receptors (IC50s = 27.5 and 2,239, 3,162 and >10,000, 5,623, and 10,000 nM, respectively). Nebivolol inhibits cAMP accumulation induced by norepinephrine in primary rat cardiac cells (IC50= 22 nM) and induces vasodilation in mouse renal arteriesviaa nitric oxide- and cGMP-dependent mechanism (EC50= 11.36 μM).2,3It decreases contraction of isolated human left ventricular trabeculae induced by isoproterenol but does not exert intrinsic sympathomimetic activity (ISA).4Nebivolol inhibits proliferation of human coronary artery smooth muscle cells (HCASMCs) in the presence and absence of growth factors (IC50s = 6.1, 6.8, 6.4, and 7.7 μM for HCASMCs grown in media containing no growth factor, PDGFBB, basic FGF, and TGF-β1, respectively).5Formulations containing nebivolol have been used to treat hypertension.
1.Pauwels, P.J., Gommeren, W., Van Lommen, G., et al.The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various beta-adrenergic blockersMol. Pharmacol.34(6)843-851(1988) 2.Pauwels, P.J., Leysen, J.E., and Janssen, P.A.β-adrenoceptor-mediated cAMP accumulation in cardiac cells: Effects of nebivololEur. J. Pharmacol.172(6)471-479(1989) 3.Georgescu, A., Pluteanu, F., Flonta, M.L., et al.Nebivolol induces a hyperpolarizing effect on smooth muscle cells in the mouse renal artery by activation of beta-2-adrenoceptorsPharmacology81(2)110-117(2008) 4.Brixius, K., Bundkirchen, A., BÖlck, B., et al.Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardiumBr. J. Pharmacol.133(8)1330-1338(2001) 5.Brehm, B.R., Wolf, S.C., Bertsch, D., et al.Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cellsCardiovasc. Res.49(2)430-439(2001)