Ellis K M, Cannet C, Mazzoni L, Fozard J R
Research Department, Novartis Institute for Biomedical Research, 4002 Basel, Switzerland.
Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):166-78. doi: 10.1007/s00210-003-0857-6. Epub 2004 Jan 15.
The mechanism(s) of bradykinin-induced bronchoconstriction was investigated in the Brown Norway (BN) rat model of allergic asthma. Bronchoconstrictor responses to i.v. bradykinin in BN rats were maximally augmented 24 h following challenge with allergen and declined at later time points. Histological evaluation of the inflammatory status of the lungs after ovalbumin (OA) challenge showed a marked inflammatory response, which was maximal at 24 h and declined thereafter. However, pretreatment with budesonide did not inhibit the augmented bronchoconstrictor response to bradykinin 24 h after allergen challenge. The selective B1 receptor agonist, Lys-[desArg9]-BK had no bronchoconstrictor effects, whereas the selective B2 receptor antagonist, HOE 140, abolished the response to bradykinin in OA-challenged animals. The augmented response to bradykinin was not affected by methysergide, indomethacin, disodium cromoglycate, iralukast, the 5-lipoxygenase inhibitor, CGS8515, or the NK2 receptor antagonist, SR48968. It was, however, partially inhibited by atropine both in saline- and OA-challenged animals. Pretreatment with captopril and thiorphan markedly potentiated responses to bradykinin both in saline- and OA-challenged animals. Thus, augmentation of the bronchoconstrictor response to bradykinin occurs in actively sensitised BN rats 24 h after challenge with OA and is associated with marked pulmonary inflammation. The response is entirely B2 receptor mediated and approximately 50% of the response is cholinergic. However, mast cell activation, the products of the cyclooxygenase or 5-lipoxygenase pathways and tachykinins are not involved. Peptidase inhibition mimics the effect of allergen challenge on the bronchoconstrictor response to bradykinin and it remains possible that the mechanism of the augmented response to bradykinin following allergen challenge involves downregulation of peptidase activity as a consequence of the inflammatory response.
在棕色挪威(BN)大鼠过敏性哮喘模型中研究了缓激肽诱导支气管收缩的机制。在变应原激发后24小时,BN大鼠对静脉注射缓激肽的支气管收缩反应最大程度增强,并在随后的时间点下降。卵清蛋白(OA)激发后对肺炎症状态的组织学评估显示出明显的炎症反应,在24小时时最大,此后下降。然而,用布地奈德预处理并不能抑制变应原激发后24小时对缓激肽增强的支气管收缩反应。选择性B1受体激动剂Lys-[desArg9]-BK没有支气管收缩作用,而选择性B2受体拮抗剂HOE 140消除了OA激发动物对缓激肽的反应。对缓激肽增强的反应不受麦角新碱、吲哚美辛、色甘酸钠、伊拉鲁卡司特、5-脂氧合酶抑制剂CGS8515或NK2受体拮抗剂SR48968的影响。然而,在生理盐水和OA激发的动物中,阿托品均能部分抑制该反应。用卡托普利和硫氧还蛋白预处理在生理盐水和OA激发的动物中均显著增强了对缓激肽的反应。因此,在OA激发的主动致敏BN大鼠中,激发后24小时对缓激肽的支气管收缩反应增强,并与明显的肺部炎症相关。该反应完全由B2受体介导,约50%的反应是胆碱能的。然而,肥大细胞活化、环氧化酶或5-脂氧合酶途径的产物以及速激肽均不参与。肽酶抑制模拟了变应原激发对缓激肽支气管收缩反应的影响,变应原激发后对缓激肽增强反应的机制仍有可能是炎症反应导致肽酶活性下调。