诺司咪唑抗过敏作用的实验研究

目的: 观察诺司咪唑(norstemizole)的抗过敏作用。方法: 采用豚鼠在体和离体实验模型, 观察诺司咪唑的抗过敏效应。结果: 诺司咪唑10^-9~10^-8 mol·L^-1, 能抑制磷酸组胺引起的豚鼠离体回肠平滑肌的收缩, IC50为4.42 ×10^-9 mol·L^-1 。豚鼠口服诺司咪唑0.1, 0.5 和1.0 mg·kg^-1 3 个剂量, 均可显著地抑制磷酸组胺所致的休克作用和皮肤血管通透性增加(P<0.01)。在大鼠同种被动皮肤过敏(PCA)模型中, 能显著地抑制其皮肤过敏, 抑制率分别为23.6 %, 67.9 %和81.7 %。结论: 诺司咪唑为第三代抗组胺药, 在药效上优于母体化合物阿司咪唑。

Experiment study on antiallergic effects of norstemizole

AIM: To study the antiallerergic effects of norastemizole.METHODS: Antiallergic effects of norastemizole were study using rats and guinea pigs.RESULTS: Norastemizole (10^-9-10^-8 mol·L^-1) caused inhibition effect on the hisitamine-induced contraction of isolated guinea pig ileum.Its IC50 was 4.42 ×10^-9mol·L^-1.Norastemizole at oral doses of 0.1, 0.5,1 mg·kg^-1, norastemizole caused a significant inhibition on the histamin-phosphate induced shock in guinea pigs (P<0.01).At doses of 0.5, 1.0 and 2.0 mg·kg^-1, it significantly inhibited homologous PCA (P<0.01).At oral doses of 0.05, 0.5 and 1.0 mg·kg^-1, norastemizole caused a significant inhibition on the increase of skin vascular permeability induced by histamine.CONCLUSION: Norastemizole is a third-generation antihistamine drug, and shows significant advantages over the parent compound astemizole in potency.