货号 | 15228-50mg |
描述 | Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated (HCN) channels contribute to native pacemaker currents in heart and neurons and modulate cardiac and neuronal excitability.1 Certain HCN channels also accentuate neuropathic pain.2 ZD 7288 is a potent blocker of HCN channels that inhibits HCN4 more potently than HCN1 (IC50s = 32 and 158 nM, respectively).3 Through its effects on HCN channels, ZD 7288 modulates the sinoatrial node and slows heart rate.4,5 In addition, ZD 7288 reduces neuropathic pain in several animal models.6,7 |
别名 | ICI-D 7288; |
供应商 | Cayman |
应用文献 | |
1.Herrmann, S.,Schnorr, S. and Ludwig, A. HCN channels-modulators of cardiac and neuronal excitability. Int.J.Mol.Sci 16, 1429-1447 (2015). 2.Wickenden, A.D.,Maher, M.P. and Chaplan, S.R. HCN pacemaker channels and pain: A drug discovery perspective. Current Pharmaceutical Design 15, 2149-2168 (2009). 3.McClure, K.J.,Maher, M.,Wu, N., et al. Discovery of a novel series of selective HCN1 blockers. Bioorganic & Medicinal Chemistry Letters 21, 5197-5201 (2011). 4.BoSmith, R.E.,Briggs, I. and Sturgess, N.C. Inhibitory actions of ZENECA ZD7288 on whole-cell hyperpolarization activated inward current (If) in guinea-pig dissociated sinoatrial node cells. British Journal of Pharmacology 110(1), 343-349 (1993). 5.Rouse, W. and Johnson, I.R. Haemodynamic actions of a novel sino-atrial node function modulator, ZENECA ZD7288, in the anaesthetized dog: A comparison with zatebradine, atenolol and nitrendipine. British Journal of Pharmacology 113(3), 1064-1070 (1994). 6.Luo, L.,Chang, L.,Brown, S.M., et al. Role of peripheral hyperpolarization-activated cyclic nucleotidemodulated channel pacemaker channels in acute and chronic pain models in the rat. Neuroscience 144, 1477-1485 (2007). 7.Chen, Y.,Lin, C.,Tang, Y., et al. ZD 7288, an HCN channel blocker, attenuates chronic visceral pain in irritable bowel syndrome-like rats. World Journal of Gastroenterology 20(8), 2091-2097 (2014). | |
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 | 292.8 |
分子式 | C15H21N4 • Cl |
CAS号 | 133059-99-1 |
稳定性 | ≥ 2 years |
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