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目的 :研究滨蒿内酯 (Scoparone,Sco)对豚鼠离体气管平滑肌张力的影响。方法 :制备豚鼠离体气管环标本 ,通过测定其张力变化 ,观察 Sco对离体气管平滑肌的舒张作用及与组胺 (His)、乙酰胆碱 (Ach)、普萘洛尔(Pro)之间的相互作用。结果 :Sco可剂量依赖性地舒张气管平滑肌 ,PD2 值为 5 .2 2± 0 .13;Sco使 His收缩气管平滑肌的量效曲线下移 ,显示非竞争性抑制作用 ,PD2 ’值为 4.5 4± 0 .41;Sco(5μmol/L ,10μm ol/L )对 Ach收缩气管平滑肌的量效曲线无明显影响 ;Pro(0 .1μm ol/L ,1μmol/L )对 Sco舒张气管平滑肌的量效曲线无明显影响 ;Sco对His诱发的气管平滑肌依内钙性收缩有显著的抑制作用 (P <0 .0 1) ,对 His诱发的依外钙性收缩无抑制作用。结论 :Sco可直接舒张豚鼠离体气管平滑肌 ,此效应的发生可能与 M3或β2 受体无关 ,但 Sco与 H1 受体存在着非竞争性抑制关系 ;Sco可显著抑制 His诱发的豚鼠气管平滑肌依内钙性收缩 ,为 Sco抑制 His收缩效应的主要机制。
Objective: To study the effect of Scoparone (Sco) on the tension of isolated tracheal smooth muscle in guinea pigs. METHODS: The guinea pig isolated tracheal ring specimens were prepared and the tension of the isolated trachea smooth muscles was observed by observing the tension changes of the guinea pig. The interactions between histamine (His), acetylcholine (Ach) and propranolol (Pro) were observed. effect. Results: Sco can relax the trachea smooth muscle in a dose-dependent manner, with a PD2 value of 5.22 ± 0.13. Sco reduced the dose-response curve of His-constricted tracheal smooth muscle to a non-competitive inhibition. The PD2’ value was 4.5 4 ± 0 .41; Sco (5 μmol/L, 10 μmol/L) had no significant effect on the dose-response curve of Ach-constricted tracheal smooth muscle; Pro (0.1 μg ol/L, 1 μmol/L) was effective for Sco dilation of tracheal smooth muscle. There was no significant effect of the curve; Sco significantly inhibited intranasal calcium contraction induced by His (P < 0.01), and had no inhibitory effect on His-induced extraneous calcium contraction. Conclusion: Sco can directly relax guinea pig isolated tracheal smooth muscle. This effect may not be related to M3 or β2 receptors, but there is a non-competitive inhibitory relationship between Sco and H1 receptors; Sco can significantly inhibit the His-induced guinea pig tracheal smooth muscle. Intracellular calcium contraction is the main mechanism by which Sco inhibits the contractile effect of His.