塞曲司特对致喘介质诱发的豚鼠离体气管条和肺条收缩的影响

Effect of Seratrodast on Contraction of Guinea-pig Isolated Tracheal Strips and Lung Parenchyma Strips Induced by Some Asthmagenic Meditors

目的 在体外研究血栓素A2 受体拮抗剂塞曲司特对组胺、乙酰胆碱、KCl诱发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 受体激动剂沙丁胺醇比较。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 )用沙丁胺醇孵育前后组胺、KCl诱发的豚鼠离体气管条的收缩 ;(3)塞曲司特、沙丁胺醇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 ,塞曲司特抑制了组胺、乙酰胆碱诱发的收缩 ;(2 )对6 0mmol/LKCl诱发的气管条收缩 ,塞曲司特、沙丁胺醇均可抑制其最大收缩反应 ;(3)对组胺诱导的肺条收缩 ,塞曲司特、沙丁胺醇均明显拮抗了其收缩。结论 塞曲司特对致喘介质诱发的豚鼠离体气管条和肺条收缩有明显的抑制作用 。

Purpose: To study the inhibitory effect of thromboxane A2 receptor antagonist, 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 to compare it with short-acting β2-receptor agonist salbutamol. Methods: The following were measured and recorded by quantitative pharmacologic: (1) The contraction of guinea-pig tracheal strips induced by His, Ach and KCl before and after being incubated with seratrodast; (2) The contraction of guinea-pig tracheal strips induced by His, and KCl before and after being incubated with salbutamol; (3) the inhibitory effect of seratrodast and salbutamol on the contraction of guinea pig lung parenchyma strips induced by histamine. Results: (1) His, Ach caused concentration-related contraction on the tracheal strips in vitro, seratrodast inhibited the contraction of tracheal strips induced by His, Ach; (2) Seratrodast and salbutamol inhibited the maximal contraction response induced by 60 mmol/L KC1; (3) Seratrodast and salbutamol 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 meditors. It is an effective bronchodilator.