Product Data SheetProduct Name:CAS No.: CtNCat. No.:MWt:Formula:Purity :Nitrendipine39562-70-4HYB0424HY-B0424360.36C18H20N2O6>98%Solubility:DMSO2DMSO 72 mg/mL; Water <1 mg/mL/LW1/LMechanisms: Pathways:Membrane Tranporter/Ion Channel; Target:Calcium Channel Biological Activity:Nitrendipine is a calcium channel blocker with marked vasodilator action. Target: Calcium Channel Nitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primaryhypertension to decrease blood pressure. Nitrendipine blocked Ca2+ currents very potently, withhalf-block by subnanomolar concentrations. The concentration dependence of block had the formexpected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM. In contrast, whencells were held at hyperpolarized potentials, nitrendipine blocked Ca2+ currents much less potently(Kd approximately equal to 700 nM) [1, 2]. Nitrendipine, a potent analogue of nifedipine, binds in areversible and saturable manner to partially purified guinea-pig heart membranes [3].[3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response[4]. References:[1]. Bean, B.P., Nitrendipine block of cardiac calcium channels: high-affinity binding to theinactivated state. Proc Natl Acad Sci U S A, 1984. 81(20): p. 6388-92. [2]. Peterson, B.Z., T.N. Tanada, and W.A. Catterall, Molecular determinants of high affinitydihydropyridinebindinginL-typedihydropyridine binding in Ltype calcium channels. J Biol Chem, 1996. 271(10): p. 5293calciumchannelsJBiolChem1996271(10):p5293-66. [3]. Bellemann, P., et al., [3H]-Nitrendipine, a potent calcium antagonist, binds with high affinity tocardiac membranes. Arzneimittelforschung, 1981. 31(12): p. 20-7. [4]. Bolger, G.T., et al., Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine,to guinea-pig ileal smooth muscle. J Pharmacol Exp Ther, 1983. 225(2): p. 291-309. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 080,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
