塞曲司特对致喘递质诱导的豚鼠气管条和肺条收缩作用的影响

Effect of thromboxane receptor antagonist on contraction of guinea pig isolated tracheal strips and lung parenchyma strips induced by some asthmagenic mediators

目的:探讨血栓素A2受体拮抗剂塞曲司特对组胺、乙酰胆碱、KCl诱导的豚鼠离体气管条和肺条收缩作用的抑制影响,并与短效β2受体激动剂特布他林比较。方法:用定量药理分析方法测定和记录:①用塞曲司特孵育前后组胺、乙酰胆碱、KCl诱发的豚鼠离体气管条的收缩;②用特布他林孵育前后组胺、乙酰胆碱、KCl诱发的豚鼠离体气管条的收缩;③塞曲司特、特布他林对组胺诱导的豚鼠肺条收缩的影响。结果:①组胺、乙酰胆碱在体外引起了豚鼠离体气管条的浓度依赖性的收缩,pD2分别为(6.19±0.47)和(5.99±0.21),塞曲司特抑制了组胺、乙酰胆碱诱发的收缩,pD2'分别为(4.16±0.82)和(3.61±0.57)。②对60mmol/LKCl诱发的气管条收缩,塞曲司特、特布他林均可抑制其最大收缩反应,IC50分别为7.28×10-6mol/L、3.36×10-6mol/L。③对组胺诱导的肺条收缩,塞曲司特、特布他林均有明显的拮抗作用。结论:塞曲司特对致喘递质诱发的豚鼠离体气管条和肺条收缩有明显的抑制作用,是一种有效的支气管扩张剂。

Objective: To study the inhibitory effect of thromboxane A 2 receptor antago- nist, seratrodast (AA-2414) on the contraction of guinea pig isolated tracheal strips and lung parenchyma strips induced by histamine, acetylcholine and KCl in vitro, and compare with short-acting β 2 -receptor agonist terbutalin. Methods: The following items were mea- sured and recorded with quantitative pharmacologic nalyzed method: ①The contraction of guinea pig tracheal strips induced with His, Ach and KCl before and after being incubated with seratrodast. ② The contraction of guinea pig tracheal strips induced with His, Ach and KCl before and after being incubated with terbutalin. ③ The inhibitory effect of seratrodast and terbutalin on the contraction of guinea pig lung parenchyma strips induced by hista- mine. Results: ①His, Ach caused concentration-related contraction on the tracheal strips in vitro, the values of pD 2 wer(e6.19±0.47)an(d5.99±0.21), respectively. Seratrodast inhibited the contraction of tracheal strips induced by His, Ach values of were pD 2 '( 4.16 ±0.82)an(d3.61±0.57), respectively. ② Seratrodast and terbutalin inhibited the maximal contraction response induced by 60 mmol/L KCl, values of were IC50 7.28×10-6 mol/L and 3.36 ×10 -6 mol/L, respectively. ③ Seratrodast and terbutalin had a significant inhibitory effects on contraction of lung parenchyma strips induced by histamine. Conclusions: Seratrodast had a significant inhibitory effects on contraction of tracheal strips and lung parenchyma strips induced by asthmagenic mediators. It is an effective bronchodilator.