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Expression of CysLT2 receptors in asthma lung, and their possible role in bronchoconstriction
Tomohiko Sekioka1, Michiaki Kadode1, Masanori Fujii2
1Discovery Research Laboratories II, Department of Biology & Pharmacology, Ono Pharmaceutical Co., Ltd., Osaka, Japan; Department of Pharmacology, Kyoto Pharmaceutical University, Kyoto, Japan.
Background:
The expression and functional role of CysLT2 receptors in asthma have not been clarified. In this study, we evaluated CysLT2 receptors expression, and effects of CysLT2-and CysLT1/2-receptor antagonists on antigen-induced bronchoconstriction using isolated lung tissues from both asthma and non-asthma subjects.
Methods:
CysLT1 and CysLT2 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 CysLT1/2-receptor antagonist, montelukast, a CysLT1 receptor antagonist, and BayCysLT2RA, a CysLT2 receptor-specific antagonist.
Results:
CysLT1 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 CysLT2 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 leukocytes in 2 in 2 asthma subjects. In the non-asthma specimens, antagonism of CysLT2 receptors did not affect antigen-induced bronchial contractions, even after pretreatment with the CysLT1-receptor specific antagonist, montelukast. However, in the bronchus isolated from one of the 2 asthma subjects, antagonism of CysLT2 receptors suppressed contractions, and dual antagonism of CysLT1 and CysLT2 receptors resulted in additive inhibitory effect on anaphylactic contractions.
Conclusions:
CysLT2 receptors were expressed in lung specimens isolated from asthma subjects. Activation of CysLT2 receptors may contribute to antigen-induced bronchoconstriction in certain asthma population.
Insights
Cysteinyl leukotriene receptor 2 (CysLT2) antagonists may help certain asthma patients by reducing antigen-induced bronchoconstriction. CysLT2 receptors are expressed in asthma lung tissues and contribute to airway hyperresponsiveness.
Area of Science:
- Pulmonary Medicine
- Immunology
- Pharmacology
Background:
- The role of Cysteinyl leukotriene receptor 2 (CysLT2) in asthma pathogenesis remains unclear.
- Previous research has not fully elucidated the expression and function of CysLT2 receptors in asthmatic airways.
Purpose of the Study:
- To investigate the expression of CysLT1 and CysLT2 receptors in lung tissues from asthma and non-asthma subjects.
- To evaluate the functional impact of CysLT2 receptor antagonism on antigen-induced bronchoconstriction in asthma models.
Main Methods:
- Immunohistochemistry was used to examine CysLT1 and CysLT2 receptor expression in lung tissues.
- Pharmacological assessment involved using ONO-6950 (dual CysLT1/2 antagonist), montelukast (CysLT1 antagonist), and BayCysLT2RA (CysLT2 antagonist) to study bronchoconstriction.
Main Results:
- CysLT1 receptors were found in both asthma and non-asthma lung tissues.
- CysLT2 receptor expression varied in non-asthma subjects but was detected in asthma lung tissues.
- Antagonism of CysLT2 receptors suppressed antigen-induced contractions in one asthma subject, with additive effects when combined with CysLT1 antagonism.
Conclusions:
- CysLT2 receptors are expressed in lung specimens from asthma patients.
- CysLT2 receptor activation may play a role in antigen-induced bronchoconstriction in a subset of asthma patients.
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