Background: The expression and functional role of CysLT
2 receptors in asthma have not been clarified. In this study, we evaluated CysLT
2 receptors expression, and effects of CysLT
2-and CysLT
1 ⁄ 2-receptor an- tagonists on antigen-induced bronchoconstriction using isolated lung tissues from both asthma and non- asthma subjects.
Methods: CysLT
1 and CysLT
2 receptors expression in asthma and non-asthma lung tissue preparations was examined in immunohistochemistry experiments, and their functional roles in antigen-induced bronchoconstriction were assessed using ONO-6950, a dual CysLT
1 ⁄ 2-receptor antagonist, montelukast, a CysLT
1 receptor antagonist, and BayCysLT
2RA, a CysLT
2 receptor-specific antagonist.
Results: CysLT
1 receptors were expressed on the bronchial smooth muscle and epithelium, and on alveolar leukocytes in 5 in 5 non-asthma subjects and 2 in 2 asthma subjects. On the other hand, although degrees of CysLT
2 receptors expression were variable among the 5 non-asthma subjects, the expression in the asthma lung was detected on bronchial smooth muscle, epithelium and alveolar leu- kocytes in 2 in 2 asthma subjects. In the non-asthma specimens, antagonism of CysLT
2 receptors did not affect antigen-induced bronchial contractions, even after pretreatment with the CysLT
1-receptor specific antagonist, montelukast. However, in the bronchus isolated from one of the 2 asthma subjects, antag- onism of CysLT
2 receptors suppressed contractions, and dual antagonism of CysLT
1 and CysLT
2 receptors resulted in additive inhibitory effect on anaphylactic contractions.
Conclusions: CysLT
2 receptors were expressed in lung specimens isolated from asthma subjects. Acti- vation of CysLT
2 receptors may contribute to antigen-induced bronchoconstriction in certain asthma population.
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