|4-(二异丙基氨基)-2-苯基-2-(2-吡啶基)丁酰胺|CsnPharm

CAS No.: 3737-09-5

Disopyramide/丙吡胺 Catalog No. CSN21438

Synonyms: Dicorantil;SC-7031

Disopyramide can block sodium channel, it is a class IA antiarrhythmic drug.

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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 ... more >> Heart Failure Collapse <<	Phase 3	Terminated(Lack of funding)	-	United States, Arizona ... more >> 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 Collapse <<
NCT00000556	Arrhythmia At... more >>rial Fibrillation Cardiovascular Diseases Heart Diseases Collapse <<	Phase 3	Completed	-	-
NCT00589303	-	-	Terminated(Lack of funding)	-	-

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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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9457 mL
- 14.7286 mL
- 29.4573 mL
- 5 mM
- 0.5891 mL
- 2.9457 mL
- 5.8915 mL
- 10 mM
- 0.2946 mL
- 1.4729 mL
- 2.9457 mL

技术信息

CAS号

3737-09-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H29N3O

运输

蓝冰

分子量

339.47

别名

Dicorantil;SC-7031

溶解度

DMSO	540.0 mg/mL (1590.7 mM)
Water	insoluble

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Disopyramide/丙吡胺 Catalog No. CSN21438

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