西替利嗪的抗组胺H_1受体作用  

Inhibitory effects of cetirizine on histamine H_1 receptor

作　　者：任先达[1] 杨延秀[1] 罗焕敏[1] 刘建军[1] 熊爱华[1] 钟玲[1] 杨美玲[1] 

机构地区：[1]暨南大学药学院药理学教研室,广东广州510632

出　　处：《暨南大学学报（自然科学与医学版）》2001年第6期14-17,共4页Journal of Jinan University(Natural Science & Medicine Edition)

摘　　要：目的 :观察西替利嗪的抗组胺H1受体作用。方法 :采用离体气管环试验分析pA2 ,以小鼠皮肤通透性试验和组胺致休克试验观察药效。结果 :西替利嗪 10 - 7～ 10 - 6mol·L- 1可剂量依赖性地对抗组胺引起的气管环收缩 ,使组胺的量效曲线平行右移 ,pA2 为 7.3781,西替利嗪 0 0 6～0 6 0mg·kg- 1口服给药可显著对抗组胺引起的小鼠皮肤血管通透性的增高 ,使蓝染面积显著缩小 ,蓝染皮肤伊文思蓝含量显著降低 ,当组胺用量为 3.2 μg时 ,其EC50 分别为 0 .177mg·kg- 1和 0 .379mg·kg- 1。西替利嗪 0 .0 5 6～ 0 .5 0mg·kg- 1口服给药时 ,能明显减轻豚鼠静脉注射组胺所致休克反应的严重程度 ,并可显著延长豚鼠休克反应的潜伏期及降低死亡率。结论 :西替利嗪为一强效的竞争性H1受体阻断剂。Aim: To observe inhibitory effects of cetirizine on histamine H 1 receptor.Methods: pA 2 was determined by isolated guinea-pig trachea ring test,the capillary permeability and histamine induced shock test were carried out Results: Cetirizine at the dose of 10 -7～10 -6 mol·L -1 could inhibit the contraction of isolated guinea-pig trachea ring induced by histamine dose-dependently. The dose-response curve of histamine was shifted parallely to the right,pA 2 was 7.378 1. The capillary permeability to intracutaneous injection of histamine was potently inhibited by orally administered cetirizine ranged from 0.06 to 0.60 mg·kg -1 in guinea-pigs,blue area and the content of Evans blue obviously decreased and EC 50 of cetirizine on these response to histamine 3.2 μg were 0.177 mg·kg -1 and 0.379 mg·kg -1 respectively. The guinea-pigs were effectively decreased reaction extent of shock and prolonged latency period of shock by orally administered cetirizine ranged from 0.056 to 0.50 mg·kg -1, reduced the rate of histamine induced death.Conclusion:The cetirizine is an potent competitive H 1 receptor antagonist.

关 键 词：西替利嗪 组胺 休克 变态反应 

分 类 号：R976[医药卫生—药品] R541.64[医药卫生—药学]