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

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。

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

Aim To investigate the effect of N-n-butyl haloperidol iodide(F_2) on L-type calcium channel in rat ventricular myocytes.Methods Single ventricular cells were obtained by enzymatic dissociation.The calcium current(I_(Ca)) was recorded by the whole-cell patch clamp recording technique.Results F_2 0.1,1,10×10~(-6) mol·L~(-1) reduced I_(Ca) in a concentration dependent manner.The inhibitory rate was 40%,72%,84%,Respectively.The IC_(50) was up to 1.19×10~(-6)mol·L~(-1).F_2 up-shifted the current-voltage curve of I_(Ca) without altering the maximal activation voltage and reversal potential of I_(Ca).F_2 induced a marked leftward shift of the steady-state inactivation curves of I_(Ca),but did not affect the activation kinetics of I_(Ca).F_2 markedly shifted the curve of time-dependent recovery of I_(Ca) from steady-state inactivation to the right,prolonged the recovery time of I_(Ca) from inactivation.Conclusions F_2 inhibits L-type calcium channels in rat ventricular myocytes.