Montuschi Paolo, Sala Angelo, Dahlén Sven-Erik, Folco Giancarlo
Department of Pharmacology, Faculty of Medicine, Catholic University of the Sacred Heart, Rome, Italy.
Drug Discov Today. 2007 May;12(9-10):404-12. doi: 10.1016/j.drudis.2007.03.004. Epub 2007 Mar 23.
Leukotrienes (LTs), including cysteinyl LTs (CysLTs) and LTB(4), are potent lipid mediators that have an important pathophysiological role in asthma and allergic rhinitis. Most of the effects of CysLTs that are relevant to the pathophysiology of asthma are mediated by the activation of the CysLT(1) receptor, one of the receptor subtypes for CysLTs. LTB(4) might be functionally involved in the development of airway hyperresponsiveness, acute and severe asthma and allergic rhinitis. CysLT(1) receptor antagonists can be given as monotherapy or in addition to inhaled glucocorticoids. The potential anti-remodeling effect of CysLT(1) receptor antagonists might be relevant for preventing or reversing airway structural changes in asthmatic patients. Here, we examine the role of LTs in asthma and allergic rhinitis, and the therapeutic implications of the pharmacological modulation of the LT pathway for allergic airway disease.
白三烯(LTs),包括半胱氨酰白三烯(CysLTs)和白三烯B4(LTB4),是强效脂质介质,在哮喘和过敏性鼻炎中具有重要的病理生理作用。与哮喘病理生理学相关的大多数CysLTs效应是由CysLT1受体激活介导的,CysLT1受体是CysLTs的受体亚型之一。LTB4可能在气道高反应性、急性重症哮喘和过敏性鼻炎的发生发展中发挥功能作用。CysLT1受体拮抗剂可作为单一疗法使用,也可与吸入性糖皮质激素联合使用。CysLT1受体拮抗剂潜在的抗重塑作用可能与预防或逆转哮喘患者气道结构改变有关。在此,我们探讨LTs在哮喘和过敏性鼻炎中的作用,以及LT途径的药理学调节对过敏性气道疾病的治疗意义。