诺司咪唑抗过敏作用的实验研究  

Experiment study on antiallergic effects of norstemizole

作　　者：刘昌孝[1] 王瑞芝[1] 刘宁[1] 李晶[1] 程晓翔[1] 

机构地区：[1]天津药物研究院新药评价研究中心,天津300193

出　　处：《中国临床药理学与治疗学》2004年第1期56-58,共3页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：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 -8mol·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 .4 2× 10 -9mol·L-1。豚鼠口服诺司咪唑 0 .1,0 .5和 1.0mg·kg-13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 .0 1)。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 2 3.6 % ,6 7.9%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。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 IC 50 was 4.42 ×10 -9 mol·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.

关 键 词：诺司咪唑 抗过敏 磷酸组胺 豚鼠离体回肠 通透性 

分 类 号：R976[医药卫生—药品] R965[医药卫生—药学]