Effects of a Novel Class III Antiarrhythmic Agent, CPUY11018, on Rat Atrial Fibrillation

被引：7
|
作者：
Guo, Xiang [1 ]
Chen, Chun-Lin [1 ]
Yang, Qian [2 ]
Yin, Yue-Miao [1 ]
You, Qi-Dong [2 ]
Tang, Yi-Qun [1 ]
机构：
[1] China Pharmaceut Univ, Res Div Pharmacol, Nanjing 210009, Peoples R China
[2] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China
来源：
DRUG DEVELOPMENT RESEARCH | 2010年 / 71卷 / 05期
关键词：
anti-arrhythmic agent; atrial fibrillation; CPUY11018; transient outward K(+) current; ultra-rapid delayed rectifier K(+) current; TRANSIENT OUTWARD; HEK-293; CELLS; MYOCYTES; CHANNELS; CURRENTS; AVE0118; DRUGS;
D O I：
10.1002/ddr.20375
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
CPUY11018 has anti-atrial fibrillation (AF) effects in rats. The effects of CPUY11018 on the transient outward K(+) current (I(to)) and ultra-rapid delayed rectifier K+ current (I(Kur)) were studied using whole-cell patch clamp techniques and an acetylcholine (ACh)-CaCl(2) induced AF model. CPUY11018 inhibited I(to) and I(kur) in a concentration-dependent manner with IC(50) values of 18.5 and 1.7 mu M, respectively. Inhibition was independent of the depolarizing voltage. In the AF ACh-CaCl(2) model, AF duration was effectively shortened after treatment with 5 mg/kg CPUY11018 for 4 days. These results indicate that CPUY11018 is effective in treating AF partly by blocking I(to) and I(kur). Drug Dev Res 71:303-312, 2010. (C) 2010 Wiley-Liss, Inc.
引用
收藏
页码：303 / 312
页数：10
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