Abraham William M, Scuri Mario, Farmer Stephen G
Miller School of Medicine, University of Miami at Mount Sinai Medical Center, 4300 Alton Road, Miami Beach, Florida 33140, USA.
Eur J Pharmacol. 2006 Mar 8;533(1-3):215-21. doi: 10.1016/j.ejphar.2005.12.071. Epub 2006 Feb 7.
Kinins are proinflammatory peptides that mediate a variety of pathophysiological responses. These actions occur through stimulation of two pharmacologically distinct receptor subtypes B1 and B2. In both human and animal airways, the majority of kinin-induced effects including bronchoconstriction, increases in vascular permeability and mucus secretion and cholinergic and sensory nerve stimulation appear to be bradykinin B2-receptor mediated. Peptidic and non-peptidic receptor antagonists have been developed as potential therapeutic agents. These antagonists are effective in blocking kinin-induced effects in a variety of animal models and in some instances, have been used effectively in animal models of allergic airway disease to alleviate allergen-induced pathophysiological airway responses. This review summarizes relevant studies supporting the evidence that bradykinin B2 receptor antagonism and/or upstream inhibition of tissue kallikrein will be beneficial in the treatment of inflammatory airway diseases.
激肽是介导多种病理生理反应的促炎肽。这些作用通过刺激两种药理学上不同的受体亚型B1和B2而发生。在人和动物气道中，大多数激肽诱导的效应，包括支气管收缩、血管通透性增加、黏液分泌以及胆碱能和感觉神经刺激，似乎都是由缓激肽B2受体介导的。肽类和非肽类受体拮抗剂已被开发为潜在的治疗药物。这些拮抗剂在多种动物模型中能有效阻断激肽诱导的效应，在某些情况下，已在过敏性气道疾病动物模型中有效用于减轻过敏原诱导的病理生理气道反应。本综述总结了相关研究，支持缓激肽B2受体拮抗和/或组织激肽释放酶的上游抑制在炎症性气道疾病治疗中有益的证据。
