中国药理学与毒理学杂志
中國藥理學與毒理學雜誌
중국약이학여독이학잡지
CHINESE JOURNAL OF PHARMACOLOGY AND TOXICOLOGY
2002年
6期
438-442
,共5页
李泱%傅丽英%姚伟星%夏国瑾%江明性
李泱%傅麗英%姚偉星%夏國瑾%江明性
리앙%부려영%요위성%하국근%강명성
苄基四氢巴马汀%钾通道%慢激活延迟整流钾电流%膜片钳技术%心肌
芐基四氫巴馬汀%鉀通道%慢激活延遲整流鉀電流%膜片鉗技術%心肌
변기사경파마정%갑통도%만격활연지정류갑전류%막편겸기술%심기
benzyltetrahydropalmatine%potassium channels%slowly activating component of delayed rectifier potassium current%patch clamp technique%myocardium
目的研究苄基四氢巴马汀(BTHP)的抗心律失常机理.方法采用全细胞膜片钳技术记录心室肌细胞慢激活延迟整流钾电流(IKs)及其尾电流(IKs,tail).结果 BTHP在1~100 μmol*L-1的范围内以浓度依赖性、电压依赖性和频率依赖性方式阻滞IKs,tail,其IC50为9.3 μmol*L-1(95%可信限:7.8~11.8 μmol*L-1).BTHP 30 μmol*L-1可使IKs及IKs,tail分别降低(40±6)%和(39±5)% (P<0.01).BTHP可以抑制IKs,tail.该药主要使IKs,tail的失活时间常数缩短,从而使IKs,tail失活速度增加,而对IKs,tail的激活动力学影响不大.结论 BTHP对IKs有明显的抑制作用.
目的研究芐基四氫巴馬汀(BTHP)的抗心律失常機理.方法採用全細胞膜片鉗技術記錄心室肌細胞慢激活延遲整流鉀電流(IKs)及其尾電流(IKs,tail).結果 BTHP在1~100 μmol*L-1的範圍內以濃度依賴性、電壓依賴性和頻率依賴性方式阻滯IKs,tail,其IC50為9.3 μmol*L-1(95%可信限:7.8~11.8 μmol*L-1).BTHP 30 μmol*L-1可使IKs及IKs,tail分彆降低(40±6)%和(39±5)% (P<0.01).BTHP可以抑製IKs,tail.該藥主要使IKs,tail的失活時間常數縮短,從而使IKs,tail失活速度增加,而對IKs,tail的激活動力學影響不大.結論 BTHP對IKs有明顯的抑製作用.
목적연구변기사경파마정(BTHP)적항심률실상궤리.방법채용전세포막편겸기술기록심실기세포만격활연지정류갑전류(IKs)급기미전류(IKs,tail).결과 BTHP재1~100 μmol*L-1적범위내이농도의뢰성、전압의뢰성화빈솔의뢰성방식조체IKs,tail,기IC50위9.3 μmol*L-1(95%가신한:7.8~11.8 μmol*L-1).BTHP 30 μmol*L-1가사IKs급IKs,tail분별강저(40±6)%화(39±5)% (P<0.01).BTHP가이억제IKs,tail.해약주요사IKs,tail적실활시간상수축단,종이사IKs,tail실활속도증가,이대IKs,tail적격활동역학영향불대.결론 BTHP대IKs유명현적억제작용.
AIM To clarity the antiarrhythmic mechanisms of benzyltetrahydropalmatine (BTHP). METHODS Delayed rectifier potassium current (IKs) was recorded by using whole-cell patch clamp technique. RESULTS IKs was blocked by BTHP (1-100 μmol*L-1) in concentration-, voltage- and frequency-dependent fashion with an IC50 9.3 μmol*L-1 (95% confidence range: 7.8-11.8 μmol*L-1). BTHP 30 μmol*L-1 reduced IKs and its tail current(IKs,tail) by (40±6)% and (39±5)% (P<0.01). Time constants of deactivation of IKs,tail were reduced by BTHP, with accelerating deactivation course of IKs,tail. CONCLUSION BTHP inhibited IKs in isolated guinea pig ventricular myocytes.