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采用离体豚鼠回肠试验分析pA2以及观察西替利嗪对组胺致大鼠皮肤血管通透性增高和致豚鼠休克的影响。结果表明:西替利嗪竞争性拮抗H1受体,pA2为7.17,95%可信限为7.17±0.69;西替利嗪明显对抗组胺引起的皮肤血管通透性的增高,大、中、小剂量组的作用均优于扑尔敏;其显著延长组胺静注致豚鼠呼吸加快的潜伏期,大、中剂量组的作用优于扑尔敏,小剂量组与扑尔敏相当,且可完全阻止组胺休克的发生。结果提示:西替利嗪为一强效竞争性H1受体阻断剂。
In vitro guinea pig ileum test analysis of pA2 and observe the effect of cetirizine on histamine-induced rat skin vascular permeability and guinea pig shock. The results showed that cetirizine competitively antagonized the H1 receptor with a pA2 of 7.17 and a 95% confidence limit of 7.17 ± 0.69. Cetirizine significantly counteracted histamine-induced cutaneous vascular permeability The effects of high, medium, medium and low dose groups were better than that of chlorpheniramine. It significantly prolonged the latent period of respiratory acceleration caused by intravenous injection of histamine. The effect of large dose and medium dose groups was better than chlorpheniramine, Ermin is quite, and can completely prevent the occurrence of histamine shock. The results suggest that: Cetirizine is a potent competitive H1 receptor blocker.