货号 | 14288-1g |
描述 | Verapamil is the prototypical blocker of L-type calcium channels that produces excitation-contraction uncoupling in cardiac muscle by preventing the slow-inward current of calcium ions.1 Verapamil can also block calcium fluxes in vascular smooth muscle. It has both peripheral and coronary vasodilator effects (IC50 = 0.38 μM in guinea pig aortic strip) and has been used to control hypertension, angina, cardiac arrhythmia, and vascular headaches.2,3,4 Verapamil has also been used in cell biology as an inhibitor of drug efflux pump proteins such as P-glycoprotein, which are often over-expressed in certain tumor cell lines.5 |
别名 | NSC 272366;NSC 657799; |
供应商 | Cayman |
应用文献 | |
1.Singh, B.N. The mechanism of action of calcium antagonists relative to their clinical applications. Br. J. Clin. Pharmacol. 21, 109S-121S (1986). 2.Dei, S.,Romanelli, M.N.,Scapecchi, S., et al. Verapamil analogues with restricted molecular flexibility: Synthesis and pharmacological evaluation of the four isomers of α-[1-[3-[N-[1-[2-(3,4-dimethoxy-phenyl)ethyl]]-N-methylamino]cyclohexyl]]-α-isopropyl-3,4-dimethoxybenzene-acetonitrile. Journal of Medicinal Chemistry 36, 439-445 (1993). 3.Dawson, J.R.,Whitaker, N.H.G. and Sutton, G.C. Calcium antagonist drugs in chronic stable angina. Comparison of verapamil and nifedipine. British Heart Journal 46, 508-512 (2013). 4.Campbell, T.J. and Williams, K.M. Therapeutic drug monitoring: Antiarrhythmic drugs. British Journal of Clinical Pharmacology 46, 307-319 (1998). 5.Rabindran, S.K.,He, H.,Singh, M., et al. Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C. Cancer Research 58, 5850-5858 (1998). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 491.1 |
分子式 | C27H38N2O4 • HCl |
CAS号 | 152-11-4 |
稳定性 | ≥ 2 years |
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