Pricing updated 2018-06-23. Prices are subject to change without notice.
The cysteinyl leukotrienes (CysLTs; LTC4, LTD4, and LTE4) contract airway and pulmonary vascular smooth muscle, increase vascular permeability, and stimulate mucus secretion, thereby playing a major role in asthma.1,2,3,4 LTC4, LTD4, and LTE4 mediate their actions via at least two receptors designated CysLT1 and CysLT2.1 Cloning of the human CysLT1 receptor reveals it is a 337 amino acid protein with a calculated molecular mass of 38,549.5 The rank order of binding for leukotrienes to the cloned receptor, as determined using a radioligand binding assay, is LTD4 >> LTC4 = LTE4 >> LTB4.5 The mRNA for the human CysLT1 receptor is expressed in spleen and peripheral blood leukocytes with smaller amounts in lung, placenta, and small intestine. Immunohistochemical studies reveal the receptor is expressed on eosinophils, mast cells, macrophages, neutrophils, and vascular endothelial cells in the nasal mucosa.6
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1. Gorenne, I., Norel, X., and Brink, C. Cysteinyl leukotriene receptors in the human lung: What’s new? Trends in Pharamacological Sciences 17, 342-343 (1996).
2. Dahlén, S.E., Hansson, G., Hedqvist, P., et al. Allergen challenge of lung tissue from asthmatics elicits bronchial contraction that correlates with the release of leukotrienes C4, D4, and E4. Proceedings of the National Academy of Sciences of the United States of America 80, 1712-1716 (1983).
3. Busse, W.W. The role of leukotrienes in asthma and allergic rhinitis. Clinical and Experimental Allergy 26, 868-879 (1996).
4. Hedqvist, P., Dahlén, S.E., Gustafsson, L., et al. Biological profile of leukotrienes C4 and D4. Acta Physiologica Scandinavica 110, 331-333 (1980).
5. Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399, 789-793 (1999).
6. Shirasaki, H., Kanaizumi, E., Watanabe, K., et al. Expression and localization of the cysteinyl leukotriene 1 receptor in human nasal mucosa. Clinical and Experimental Allergy 32, 1007-1012 (2002).