药学学报
藥學學報
약학학보
ACTA PHARMACEUTICA SINICA
2004年
7期
509-513
,共5页
程岚%王芳%周红义%姚伟星%夏国瑾%江明性
程嵐%王芳%週紅義%姚偉星%夏國瑾%江明性
정람%왕방%주홍의%요위성%하국근%강명성
阿米洛利%膜片钳技术%钾电流%钙电流
阿米洛利%膜片鉗技術%鉀電流%鈣電流
아미락리%막편겸기술%갑전류%개전류
amiloride%patch-clamp technique%potassium current%calcium current
目的研究阿米洛利(amiloride)对豚鼠心肌细胞钾电流及钙电流的作用.方法采用全细胞膜片钳技术记录豚鼠心室肌细胞钾通道及钙通道电流.结果阿米洛利在10~100μmol·L-1抑制L型及T型钙电流,不改变钙电流I-V曲线的形状,仅抑制这两型电流的幅度.当累积浓度达l00μmol·L-1时,阿米洛利轻微抑制快激活延迟整流钾电流(IKr),对慢激活延迟整流钾电流(IKs)无影响.阿米洛利在1~100μmol·L-1浓度依赖性地抑制内向整流钾电流(IK1).结论阿米洛利抑制电压依赖性的钾、钙电流,为其抗心律失常作用提供了离子基础.
目的研究阿米洛利(amiloride)對豚鼠心肌細胞鉀電流及鈣電流的作用.方法採用全細胞膜片鉗技術記錄豚鼠心室肌細胞鉀通道及鈣通道電流.結果阿米洛利在10~100μmol·L-1抑製L型及T型鈣電流,不改變鈣電流I-V麯線的形狀,僅抑製這兩型電流的幅度.噹纍積濃度達l00μmol·L-1時,阿米洛利輕微抑製快激活延遲整流鉀電流(IKr),對慢激活延遲整流鉀電流(IKs)無影響.阿米洛利在1~100μmol·L-1濃度依賴性地抑製內嚮整流鉀電流(IK1).結論阿米洛利抑製電壓依賴性的鉀、鈣電流,為其抗心律失常作用提供瞭離子基礎.
목적연구아미락리(amiloride)대돈서심기세포갑전류급개전류적작용.방법채용전세포막편겸기술기록돈서심실기세포갑통도급개통도전류.결과아미락리재10~100μmol·L-1억제L형급T형개전류,불개변개전류I-V곡선적형상,부억제저량형전류적폭도.당루적농도체l00μmol·L-1시,아미락리경미억제쾌격활연지정류갑전류(IKr),대만격활연지정류갑전류(IKs)무영향.아미락리재1~100μmol·L-1농도의뢰성지억제내향정류갑전류(IK1).결론아미락리억제전압의뢰성적갑、개전류,위기항심률실상작용제공료리자기출.
Aim To elucidate the possible mechanisms underlying antiarrhythmia of the non-selective Na*/H + exchanger inhibitor- amiloride. Methods Single ventricular cells were isolated using a double-enzyme method. Effects of amiloride on voltage-dependent potassium and calcium currents in isolated guinea pig ventricular myocyte were recorded by using whole-cell patch clamp techniques. Results Amiloride resulted in a concentration-dependent inhibition of peak ICa,L, But amiloride did not change the shape of their I - V curves. It only decreased the amplitudes of the currents of the two types. When Amiloride depressed potassium and calcium currents, which may give support to its uses in some diseases of the cardiovascular system.