碘化N-正丁基氟哌啶醇对大鼠心室肌细胞L型钙通道的阻断作用

Inhibitory effects of N-n-butyl haloperidol iodide on L-type calcium channel in rat ventricular myocytes

目的研究碘化N-正丁基氟哌啶醇(F2)对大鼠心室肌细胞L-型钙通道(ICa)的影响。方法采用酶急性分离的单个大鼠心室肌细胞,应用膜片钳全细胞记录技术,观察F2对ICa的影响。结果F20.1,1,10×10-6mol.L-1可剂量依赖地抑制ICa,抑制率分别为40%,72%,84%,IC50为1.19×10-6mol.L-1。F2上移ICa的I-V曲线,但不改变ICa的最大锋电位和翻转电位;F2对ICa稳态激活曲线无明显改变;F2可使得ICa稳态失活曲线左移;延长ICa失活恢复时间。结论F2对心肌细胞ICa具有阻断作用。

Aim To investigate the effect of N-n-butyl haloperidol iodide （F2 ） on L-type calcium channel in rat ventricular myocytes. Methods Single ventricular cells were obtained by enzymatic dissociation. The calcium current （Ica） was recorded by the whole-cell patch clamp recording technique. Results F2 0.1,1, 10 × 10^-6 mol . L^-1 reduced Ica in a concentration dependent manner. The inhibitory rate was 40% ,72% 84%, Respectively. The IC50 was up to 1.19 × 10^-6 mol . L^-1. F2 up-shifted the current-voltage curve of Ic, without altering the maximal activation voltage andreversal potential of Ic,. F2 induced a marked leftward shift of the steady-state inactivation curves of Ica, but did not affect the activation kinetics of Ica. F2 markedly shifted the curve of time-dependent recovery of Ica from steady-state inactivation to the right, prolonged the recovery time of Ica from inactivation. Conclusions F2 inhibits L-type calcium channels in rat ventricular myocytes.