【摘要】 目的本实验旨在观察萘哌地尔衍生物YM01的扩血管作用,评价其心血管的药理活性。方法应用血管平滑肌等张收缩的方法观察YM01对去甲肾上腺素(noradrenaline,NA)和高钾所致的血管条收缩的抑制作用以及细胞内游离钙(Ca2+)的水平的影响。结果在离体兔胸主动脉血管条,YM013×10-5mol·L-1及10-4mol·L-1对NA诱导的血管平滑肌收缩的抑制作用明显强于对高钾诱导的血管平滑肌收缩的抑制作用。YM0110-5mol·L-1对NA的量效曲线呈非竞争性拮抗作用,使该量效曲线呈非平行右移,最大反应高度压低,而钾的作用则不明显,其pD2′值为5.16。结论①萘哌地尔衍生物YM01有明显的降压作用,YM01具有与其母核NAF类似的心血管药理作用;②YM01不是典型的α受体阻滞剂。更多还原

【Abstract】 Objective To observe the vasodilative effects of YM01, a derivative of Naftopidil(NAF), in spiral strips of rabbit aorta , and evaluate the potential availability of YM01 as new drug.Methods The isotonic contraction of the thoracic aorta strips of rabbit was recorded and the changes of the intracellular calcium ([Ca 2+ ]i) level, which was elevated induced by NA and high potassium.Results In rabbit thoracic aorta strips, YM01 3×10 -5 ,10 -4 mol·L -1 inhibited the contraction induced by noradrenaline (NA) was more strong than that induced by high KCl,YM01 at 10 -5 mol·L -1 shifted the does-response curve of NA to right nonparallely, and the maximum response was decreased. However, it had little effect on the dose-response curve of KCl.Conclusions These results suggested that YM01, a derivative of NAF vasodilative effects, which maybe obtained by inhibiting α-adrenoceptor, blocking calcium channel.更多还原