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目的 探讨洛土辛(Lot)对心肌动作电位(AP)及犬浦肯野纤维(PF)慢内向电流(Isi)的影响和其在正性肌力效应中所起的作用。方法 采用标准微电极及双微电极电压钳技术。结果 Lot1~100μmol·L-1可剂量依赖性地延长豚鼠乳头肌状快反应AP的APD20和APD90,增加收缩力(Fc);在利血平化豚鼠乳头状肌,Lot对APD20和Fc的影响较未经Res化组减弱。在豚鼠左房肌,Lot30μmol·L-1可明显地削弱Ach缩短APD50和降低Fc的作用。Lot3~100μmol·L-1可剂量依赖性地增加高K+去极化诱发的豚鼠乳头状肌及兔窦房结慢反应AP的APA、Vmax;对兔APD50和窦房结周长(Sinuscyclelength,SCL)却无明显影响。在犬PF,Lot30μmol·L-1时间依赖性及剂量依赖性地(3~100μmol·L-1)增加Isi。结论 Lot有延长APD和促钙内流作用,且在其正性肌力效应的产生中起着重要作用,而这些作用的产生与其抑制PDEⅢ有关。
Objective To investigate the effect of Lotusin on myocardial action potential (AP) and canine Purkinje fiber (PF) slow inward current (Isi) and its role in positive inotropic effect. Methods Standard microelectrode and double microelectrode voltage clamp technique were used. Results Lot 1~100 μmol·L-1 dose-dependently prolonged the APD20 and APD90 of AP in guinea pig papillary muscles and increased the contractile force (Fc); the effect of Lot on APD20 and Fc in the papillary muscles of guinea pigs It is weaker than the non-Res group. In the left atrial muscle of guinea pigs, Lot 30 μmol·L-1 significantly attenuated the effect of Ach shortening APD50 and decreasing Fc. Lot 3~100 μmol·L-1 dose-dependently increased the APA, Vmax of slow-response AP in the guinea pig papillary muscles and rabbit sinus node induced by high K+ depolarization; the rabbit APD50 and sinus node length (SCL) ) But no significant effect. Isi was increased in a time-dependent and dose-dependent manner (3 to 100 μmol·L-1) in dog PF and Lot 30 μmol·L-1. Conclusion Lot has prolonged APD and calcium influx, and plays an important role in the production of inotropic effect. The production of these effects is related to the inhibition of PDEIII.