Néliat G, Ducouret P, Moreau M, Gargouïl Y M
Arch Int Pharmacodyn Ther. 1982 Feb;255(2):237-55.
The effects of butoprozine on cardiac membrane currents of frog atrial and ferret ventricular fibres were investigated in voltage clamp conditions by means of the double sucrose gap technique. Comparison was made with amiodarone and verapamil. Butoprozine was found to decrease the fast sodium and slow calcium inward currents and the delayed outward current in a dose-dependent manner. The reactivation kinetics of both inward currents were reduced by butoprozine. Amiodarone principally decreased the delayed outward current but high concentrations also depressed the inward currents. In the same way, small concentrations of verapamil inhibited the slow inward calcium current while high concentrations also affected the delayed outward and the fast inward sodium currents. The reactivation kinetics of both inward currents were reduced by amiodarone. These of the fast inward current remained unaffected by verapamil while these of the slow inward current were reduced or sometimes not appreciably changed. The effects of butoprozine on the ionic currents accounted for the modifications observed on the action potential and automaticity and this study allowed the understanding of the mechanisms by which the drug can exert its antiarrhythmic action. Some of them are common to amiodarone and verapamil.
采用双蔗糖间隙技术，在电压钳条件下研究了布托丙嗪对蛙心房肌纤维和雪貂心室肌纤维心脏膜电流的影响。并与胺碘酮和维拉帕米进行了比较。发现布托丙嗪能以剂量依赖的方式降低快钠内向电流、慢钙内向电流和延迟外向电流。布托丙嗪降低了两种内向电流的再激活动力学。胺碘酮主要降低延迟外向电流，但高浓度时也会抑制内向电流。同样，小浓度的维拉帕米抑制慢钙内向电流，而高浓度时也会影响延迟外向电流和快钠内向电流。胺碘酮降低了两种内向电流的再激活动力学。快钠内向电流的再激活动力学不受维拉帕米影响，而慢钙内向电流的再激活动力学则降低或有时无明显变化。布托丙嗪对离子电流的影响解释了在动作电位和自律性方面观察到的改变，本研究有助于理解该药物发挥抗心律失常作用的机制。其中一些机制与胺碘酮和维拉帕米相同。
