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目的:研究CPU86017及左甲状腺素(Lev)影响内钙释放及钙内流引起血管平滑肌(VSM)收缩.方法:以三种大鼠胸主动脉环(VSM)收缩,比较CPU86017,苄普地尔(Bep),维拉帕米(Ver)及尼莫地平(Nim),在正常及Lev致甲亢大鼠中的抑制作用.结果:CPU86017抑制KCl收缩正常及甲亢大鼠VSM的IC50为80(36-179)及121(62-236)μmol·L-1,强度为Bep的1/10,Ver及Nim的1/100.Ver及Nim对甲亢大鼠VSM在无钙KH液中抑制活性大幅下降-86%及-95%,而CPU86017及Bep几乎无改变.CPU86017在正常及甲亢大鼠中对钙内流的抑制强度无改变.结论:CPU86017抑制大鼠VSM钙内流强于钙释放,而Lev加强二者.
OBJECTIVE: To study the effects of CPU86017 and Lev on the release of calcium and the influx of calcium to cause the contraction of vascular smooth muscle (VSM). Methods: Three kinds of rat thoracic aortic rings (VSM) were contracted. Compared with CPU86017, Bep, Ver and Nim, Inhibition in rats. Results: The IC50 of CPU86017 for inhibition of KCl contractions and hyperthyroidism in VSMCs were 80 (36-179) and 121 (62-236) μmol·L-1, respectively, with intensity of 1/10 of Bep, Ver / Nim 1 / 100. Ver and Nim on hyperthyroid rat VSM in calcium-free KH inhibition activity decreased sharply -86% and -95%, while CPU 86017 and Bep almost no change. CPU 86017 in normal and hyperthyroid rat inhibition of calcium influx intensity did not change. Conclusion: CPU86017 inhibits calcium influx in rat VSM stronger than calcium, while Lev strengthens both.