生物活性 | |||
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描述 | Disopyramide is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide possesses a non-competitive blocking action at the neuromuscular junction, which is not reversible by anticholinesterase agents. HERG tail currents recorded at -40 mV following test pulses to +30 mV were inhibited in a dose-dependent fashion by Disopyramide concentrations within the clinical range (IC50=7.23 μM)[1]. Disopyramide inhibits multiple ion channels, leading to lower Ca transients and force, and shortens action potentials, thus reducing cellular arrhythmias[2]. Disopyramide may be effective for preventing tachyarrhythmias in SQTS1 (Short QT syndrome1)-patients carrying the N588K mutation in HERG channel by APD (action potential duration)-prolongation via enhancing ICa-L (inward L-type calcium channel current), late INa (the late sodium channel current), INCX (the Na/Ca exchanger current), and reducing ISK (outward small-conductance calcium-activated potassium channel current)[3]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00589303 | Atrial Fibrillation ... 展开 >> Heart Failure 收起 << | Phase 3 | Terminated(Lack of funding) | - | United States, Arizona ... 展开 >> Mayo Clinic Arizona Scottsdale, Arizona, United States, 85259 United States, Indiana The Heart Group Evansville, Indiana, United States, 47710 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Oregon Oregon Health and Science University Portland, Oregon, United States, 97239 United States, Tennessee Chattanooga Heart Institute Chattanooga, Tennessee, United States, 37404 Canada, Alberta University of Calgary and Calgary Health Region Calgary, Alberta, Canada, T2N-4N1 收起 << |
NCT00000556 | Arrhythmia At... 展开 >>rial Fibrillation Cardiovascular Diseases Heart Diseases 收起 << | Phase 3 | Completed | - | - |
NCT00589303 | - | Terminated(Lack of funding) | - | - |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.95mL 0.59mL 0.29mL |
14.73mL 2.95mL 1.47mL |
29.46mL 5.89mL 2.95mL |
参考文献 |
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