Drazen J M
Departments of Medicine, Pulmonary Division, Harvard Medical School and Brigham and Women's Hospital, Boston, Massachusetts, USA.
Am J Respir Crit Care Med. 1998 Nov;158(5 Pt 3):S193-200. doi: 10.1164/ajrccm.158.supplement_2.13tac180.
The cysteinyl leukotrienes are potent mediators of airway narrowing derived from the lipoxygenation of arachidonic acid and the adduction of glutathione to this eicosanoid backbone. In lower animals and humans, the cysteinyl leukotrienes are among the most potent airway contractile substances ever identified. Furthermore, these moieties can be recovered from the urine during induced or spontaneous asthma attacks. Most important, inhibition of the synthesis of the leukotrienes or prevention of their action at the CysLT1 receptor is associated with an improvement in the airway dysfunction that occurs in both induced and spontaneous asthma. These data indicate that the cysteinyl leukotrienes have a clinically significant role in the airway obstruction that characterizes asthma.
半胱氨酰白三烯是由花生四烯酸经脂氧合作用以及谷胱甘肽与这种类二十烷酸主链加成反应而产生的强效气道狭窄介质。在低等动物和人类中,半胱氨酰白三烯是已发现的最强效气道收缩物质之一。此外,在诱发或自发性哮喘发作期间,这些物质可从尿液中检测到。最重要的是,抑制白三烯的合成或阻止其在半胱氨酰白三烯1型(CysLT1)受体上发挥作用,与诱发型和自发性哮喘中出现的气道功能障碍改善相关。这些数据表明,半胱氨酰白三烯在以气道阻塞为特征的哮喘中具有临床显著作用。