速激肽受体拮抗剂对豚鼠组胺反应的影响  

Effects of tachykinin receptor antagonists on the responses to histamine in guinea pigs

作　　者：陆智勇[1,2] 张纬萍[1,2] 魏尔清[1,2] 

机构地区：[1]浙江医科大学神经生物实验室 [2]日本大阪大学

出　　处：《中国药理学通报》1997年第4期315-318,共4页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金

摘　　要：目的：探讨速激肽与组胺（Ｈｉｓ）反应的关系。方法：观察速激肽受体拮抗剂对豚鼠Ｈｉｓ的整体和离体的呼吸道和心血管效应。结果：单用或合用速激肽ＮＫ－１受体拮抗剂ＣＰ－９６３４５（１ｍｇ·ｋｇ－１，ｉｐ）及ＮＫ－２受体拮抗剂ＳＲ－４８９６８（１ｍｇ·ｋｇ－１，ｉｐ）均可显著降低清醒豚鼠吸入Ｈｉｓ气雾的气道反应性。ＣＰ－９６３４５（１ｍｇ·ｋｇ－１，ｉｖ）可显著降低静脉注射Ｈｉｓ引起麻醉豚鼠支气管和心房的伊文思蓝渗出，ＳＲ－４８９６８（１ｍｇ·ｋｇ－１，ｉｖ）则对肺内压升高有较弱的抑制作用，两药对平均动脉压降低无明显作用。在豚鼠的离体气管和支气管平滑肌标本，ＣＰ－９６３４５（１μｍｏｌ·Ｌ－１）及ＳＲ－４８９６８（１μｍｏｌ·Ｌ－１）对Ｈｉｓ的Ｅｍａｘ及ｐＤ２无明显作用。结论：速激肽部分参与了豚鼠的Ｈｉｓ炎症反应，速激肽受体拮抗剂有抗炎作用。AIM: To investigate the relationship between tachykinins and the responses to histamine in guinea pigs. METHODS: Effects of tachykinin receptor antagonists on the airway and cardiovascular responses to histamine in guinea pigs in vivo and in vitro were observed. RESULTS: In unrestrained conscious guinea pigs, CP 96345 (1 mg·kg -1 ,ip), a specific antagonist for tachykinin NK 1 receptor, SR 48968(1 mg·kg -1 , ip), an NK 2 receptor antagonist, and combination of the both agents all attenuated airway responsiveness to histamine aerosol. In anesthetized guinea pigs, CP 96345(1 mg·kg -1 , iv) inhibited histamine induced evans blue extravasation in bronchi and atria; SR 48968(1 mg·kg -1 , iv) weakly decreased the rise of IPP induced by histamine; Neither CP 96345 nor SR 48968 had effects on the histamine induced decrease of MAP. In the isolated tracheal and bronchial smooth muscle preparations of guinea pigs, none of agents (1 μmol·L -1 , respectively) had alterd E max and pD 2 for histamine induced contraction. CONCLUSIONS: Tachykinins partially participate in the responses to histamine in guinea pigs, and tachykinin receptor antagonists could have anti inflammatory activities.

关 键 词：速激肽 受体拮抗剂 组胺反应 消炎药 

分 类 号：R971.1[医药卫生—药品]