【摘要】 目的研究色满类化合物HEF-05对兔离体血管平滑肌的舒张作用。方法以兔降主动脉为标本,加入高钾液、氯化钡诱导收缩后,累积加入HEF-05,观察HEF-05舒张作用。收缩的兔降主动脉标本,加入四乙胺（TEA）、吲哚美辛溶液分别阻断钾通道及PGs类物质合成后,累积加入HEF-05,分析HEF-05舒张作用机制与钾通道、前列腺素类物质（PGs）的关系。标本去内皮后,观察HEF-05舒张作用与内皮关系。给予不同浓度HEF-05,观察其对氯化钙量效曲线的影响。结果 HEF-05降低由高钾溶液(60 mmol·L^-1)、氯化钡(2 mg·mL^-1)收缩的兔降主动脉;经四乙胺(TEA,3×10-5 mol·L^-1)阻断后,HEF-05舒张兔降主动脉作用有明显变化;经吲哚美辛(1×10^-6 mol·L^-1)孵育或血管去内皮后,HEF-05舒张作用无显著变化。HEF-05能非竞争性抑制氯化钙收缩量效曲线。结论 HEF-05对收缩的兔降主动脉有舒张作用,其机制可能与钾通道及钙通道有关,与PGs类物质及内皮无关。更多还原

【Abstract】 Objective To determine the relaxing effect of HEF-05 on the descending aorta smooth muscle of rabbit. Methods The descending aorta of rabbits was used as the specimens, the effect of HEF-05 on agonistinduced contraction by High-K+and BaCl₂ respectively was investigated in vitro. The experimental and relaxing effect of HEF-05 on the endothelium-intact（EC +） and endothelium-denuded（EC-） thoracic aortic rings were compared. Potassium channel blockers, and COX-inhibitoers were used to explore the association between the relaxing effects of HEF-05 with potassium channels, and prostaglandin-like substances respectively. The inhibition effect of HEF-05 on the dose-effect curve of CaCl₂ was also observed. Results HEF-05 relaxed the descending aorta smooth muscle contraction by High-K+(60 mmol·L^-1) or BaCl₂(2 mg·m L^-1) in a dose-dependently way. Indomethacin(1×10⁶ mol·L^-1) had no obvious contribution to the vasorelaxant effect of HEF-05. There was no difference in the relaxing effect of HEF-05 between EC + and EC-on the thoracic aortic rings. In contrast, the vasorelaxant effect of HEF-05 was significantly inhibited by TEA(3×10-5 mol·L^-1). HEF-05 affected the doseeffect curve of CaCl₂ in a non-competitive way. Conclusion The relaxant effect of HEF-05 on the descending aorta smooth muscle might be attributed to the potassium channels and calcium channels.更多还原