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中国临床药理学与治疗学 ›› 2004, Vol. 9 ›› Issue (6): 687-690.

• 研究原著 • 上一篇    下一篇

国产盐酸氮䓬斯汀抗组胺作用的实验评价

张晓红, 吴晋湘, 胡长平1   

  1. 中南大学药学院药理学系, 长沙410078, 湖南
  • 收稿日期:2004-03-02 修回日期:2004-04-16 发布日期:2020-11-22
  • 通讯作者: 胡长平,男, 博士, 副教授, 研究方向:心血管药理学。Tel:0731-2355077 Fax:0731-2355078E-mail:huchangping2001 @yahoo.com.cn
  • 作者简介:张晓红, 女, 大学, 助理实验师, 研究方向:心血管药理学。Tel:0731-2355077  Fax :0731-2355078 E-mail:zhangxiaohongyxy@yahoo.com.cn

Experimental evaluation of the antihistamine effect of domestic azelastine hydrochloride

ZHANG Xiao-Hong, WU Jin-Xiang, HU Chang-Ping   

  1. Department of Pharmacology, School of Pharmaceutical Sciences, Central SouthUniversity, Changsha 410078, Hunan,China
  • Received:2004-03-02 Revised:2004-04-16 Published:2020-11-22

摘要: 目的 评价国产盐酸氮卓斯汀的抗组胺作用。 方法 皮内注射组胺增加豚鼠皮肤通透性;静脉注射组胺诱导豚鼠休克;组胺诱导离体豚鼠回肠平滑肌收缩。 结果 盐酸氮卓斯汀(0.05, 0.15,0.45 mg·kg-1, ig) 可剂量依赖性地抑制组胺所致皮肤血管通透性增加;盐酸氮卓斯汀(0.05, 0.1,0.2 mg·kg-1, ig) 可剂量依赖性地降低休克的反应程度, 延长休克的潜伏期, 降低豚鼠的死亡率。盐酸氮卓斯汀(10-8, 3 ×10-8, 10-7, 3 ×10-7 mol·L-1) 可剂量依赖性拮抗组胺所致离体回肠平滑肌收缩, 使组胺量效曲线平行右移(pA2 值为8.55)。 结论 国产盐酸氮卓斯汀具有较好的抗组胺作用。

关键词: 盐酸氮卓斯汀, 磷酸组胺, 休克, 血管通透性, 离体回肠, 豚鼠

Abstract: AIM: To evaluate the antihistamine effects of domestic azelastine hydrochloride. METHODS: Histamine increased skin vascular permeability and induced shock model in guinea pigs.In isolated guinea pig ileal rings, the contraction of smooth muscle induced by histamine was determined. RESULTS: Pretreament with azelastine hydrochloride(0.05, 0.15, and 0.45 mg·kg-1,ig) significantly inhibited the increase in skin vascular permeability induced by histamine in a dose-dependent manner in guinea pigs.Pretreament with azelastine hydrochloride(0.05, 0.1, and 0.2 mg·kg-1, ig) produced a significant improvement of shock, as shown by a decrease in reactivity degree, mortality and a prolongation of latency.In isolated guinea pig ileal rings, azelastine hydrochloride (10-8, 3 ×10-8, 10-7, 3 ×10-7mol·L-1) significantly inhibited contraction of smooth muscle induced by histamine in a concentration-dependent manner and caused a parallel right shift of the dose-effect curve of histamine (pA2=8.55). CONCLUSION: Domestic azelastine hydrochloride shows significant the antihistamine effects.

Key words: azelastine hydrochloride, histamine phosphate, shock, vascular permeability, isolated ileal rings, guinea pigs

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