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目的 :观察盐酸氮 艹卓 斯汀 (azelastinehydrochlo ride ,AZ)对豚鼠实验性哮喘的作用 ,并探讨其作用机制。方法 :采用组胺和乙酰胆碱诱发在体豚鼠实验性哮喘模型 ,观察AZ的整体作用 ;采用豚鼠离体气管螺旋条 ,观察AZ对组胺所致的豚鼠离体气管螺旋条痉挛的拮抗作用。结果 :AZ能够剂量依赖性地拮抗组胺和乙酰胆碱的引喘作用 ,明显延长引喘潜伏期 ,显著减少抽搐动物发生率 ,其ED50 为 0 .2 16mg·kg-1,95 %可信限为 0 .2 14～ 0 .2 19mg·kg-1。AZ可剂量依赖性地拮抗组胺对离体气管平滑肌的收缩作用 ,使组胺量效曲线平行右移 ,其pA2 值为 8.99。结论 :预先给予AZ能显著拮抗组胺和乙酰胆碱所诱发的在体豚鼠实验性哮喘 ,抑制组胺所致的气管螺旋条收缩
Objective: To observe the effect of azelastine hydrochloride (AZ) on experimental asthma in guinea pigs and to explore its mechanism. Methods: Histamine and acetylcholine were used to induce experimental asthma in guinea pigs, and the overall effect of AZ was observed. The antagonistic effect of AZ on tracheal spasm induced by histamine in guinea pigs was observed using guinea pig tracheal strips. Results: AZ could antagonize the asthmatic effect of histamine and acetylcholine in a dose-dependent manner, prolong the incubation period of asthma and significantly reduce the incidence of convulsions. The ED50 was 0.226 mg · kg-1, and the confidence limit was 0 .2 14 ~ 0 .2 19mg · kg-1. AZ antagonized the contractile effect of histamine on isolated tracheal smooth muscle in a dose-dependent manner. The histamine dose-effect curve shifted to the right parallel with a pA2 value of 8.99. CONCLUSION: AZ pretreatment can significantly antagonize histamine and acetylcholine induced experimental asthma in guinea pigs and inhibit histamine induced tracheal contraction