Inhibition of Na+/Ca2+ exchange by hexapeptide FRCRSFa in rat ventricular myocytes  

六肽FRCRSFa对大鼠心室肌Na^+/Ca^(2+)交换的抑制(英文)

作　　者：韩清华 武冬梅[1] 吕吉元[2] 吴博威[1] 

机构地区：[1]山西医科大学生理教研室,太原中国030001 [2]山西医科大学第一医院心内科,太原030001

出　　处：《Acta Pharmacologica Sinica》2002年第6期529-533,共5页中国药理学报（英文版）

基　　金：Project supported by the National Natural Science Foundation of China, № 30170346.

摘　　要：AIM: To study the effect of Phe-Arg-Cys-Arg-Ser-Phe-CONH2 (FRCRSFa) on Na+/Ca2+ exchange and its specificity in rat ventricular myocytes. METHODS: Na+/Ca2+ exchange current (INa+/ca2+ ) and other currents were measured using whole-cell voltage clamp technique. RESULTS: A concentration-dependent inhibition of hexapeptide FRCRSFa on Na+/Ca2+ exchange was observed in rat ventricular myocytes. IC50 of inward and outward INa+ Ca2+ were 2 and 4μmol/L, respectively. FRCRSFa 5 μmol/L did not affect L-type Ca2+ current, voltage-gated Na+ current, transient outward K+ current, and inward rectifier K+ current. CONCLUSION: These data indicate that FRCRSFa is an available inhibitor of Na+/Ca2+ exchange with relative selectivity and may be valuable for studies of the Na+/ Ca2+ exchange in cardiac myocytes.目的:研究六肽FRCRSFa对大鼠心室肌细胞Na^+/Ca^(2+)交换的作用及其特异性.方法:用膜片箝全细胞记录法测定Na^+/Ca^(2+)交换电流(I_(Na Ca^(2+))及其它离子通道电流.结果:六肽FRCRSFa对大鼠心室肌细胞Na^+/Ca^(2+)交换呈剂量依赖性抑制,内向和外向I_(Na^+ Ca^(2+))的IC_(50)分别是2μmol/L和4μmol/L.FRCRSFa 5μmol/L对L型钙电流,门控钠电流、瞬时外向钾电流和内向整流钾电流均无显著抑制作用.结论:FRCRSFa是一个对Na^+/Ca^(2+)交换选择性较高的抑制剂,对研究心肌细胞Na^+/Ca^(2+)交换具有较高价值.

关 键 词：FRCRSFa patch-clamp techniques Na+/Ca2+ exchanger MYOCARDIUM 

分 类 号：R96[医药卫生—药理学]