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.
出处
《中国药理学通报》
CAS
CSCD
北大核心
1997年第4期315-318,共4页
Chinese Pharmacological Bulletin
基金
国家自然科学基金
关键词
速激肽
受体拮抗剂
组胺反应
消炎药
tachykinin receptor antagonist
CP 96345
SR 48968
histamine