Disopyramide

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Chemical Structure| 3737-09-5 同义名 : 达舒平 ;SC-7031; Dicorantil; Ritmilen; (±)-Disopyramide
CAS号 : 3737-09-5
货号 : A342795
分子式 : C21H29N3O
纯度 : 99%
分子量 : 339.47
MDL号 : MFCD00057366
存储条件:

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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
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
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

[1]Jones SV, Marshall IG. Non-competitive effects of disopyramide at the neuromuscular junction: evidence for endplate ion channel block. Br J Anaesth. 1987 Jun;59(6):776-83

[2]Coppini R, Ferrantini C, Pioner JM, Santini L, Wang ZJ, Palandri C, Scardigli M, Vitale G, Sacconi L, Stefàno P, Flink L, Riedy K, Pavone FS, Cerbai E, Poggesi C, Mugelli A, Bueno-Orovio A, Olivotto I, Sherrid MV. Electrophysiological and Contractile Effects of Disopyramide in Patients With Obstructive Hypertrophic Cardiomyopathy: A Translational Study. JACC Basic Transl Sci. 2019 Oct 9;4(7):795-813

[3]Lan H, Xu Q, El-Battrawy I, Zhong R, Li X, Lang S, Cyganek L, Borggrefe M, Zhou X, Akin I. Ionic Mechanisms of Disopyramide Prolonging Action Potential Duration in Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes From a Patient With Short QT Syndrome Type 1. Front Pharmacol. 2020 Oct 12;11:554422