Leukotrienes, leukotriene receptor antagonists and leukotriene synthesis inhibitors in asthma: An update. Part I: Synthesis, receptors and role of leukotrienes in asthma
P. Devillier et al., Leukotrienes, leukotriene receptor antagonists and leukotriene synthesis inhibitors in asthma: An update. Part I: Synthesis, receptors and role of leukotrienes in asthma, PHARMAC RES, 40(1), 1999, pp. 3-13
Asthma is a chronic inflammatory disease associated with airflow obstructio
n. Airflow obstruction results from contraction of airway smooth muscle, mu
cosal oedema, increased secretion of mucus and infiltration of the airway w
all by inflammatory cells, particularly eosinophils. Leukotrienes are thoug
ht to contribute to the pathophysiology of asthma. Leukotrienes are synthes
ised from arachidonic acid by a specific synthesis pathway whose key enzyme
is 5-lipoxygenase. Cysteinyl leukotrienes (leukotrienes C-4, D-4 and E-4)
have been shown to mimic all the pathologic changes that are characteristic
of asthma, whereas leukotriene B-4 does not appear to exert biological pro
perties relevant to asthma. Cysteinyl leukotrienes bind to two receptor sub
types: CpsLT(1) and CysLT(2). Most of the biological properties of cysteiny
l leukotrienes relevant to asthma are mediated through CysLT(1) receptor st
imulation. (C) 1999 Academic Press.