Antigen: human CysLT₁ receptor C-terminal amino acids 318-337 (YVPRKKASLPEKGEEICKV) · Host: rabbit · Application(s): WB, ICC, IHC (paraffin-embedded sections), and FC · 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

1 Gorenne, I., Norel, X., and Brink, C. Cysteinyl leukotriene receptors in the human lung: What’s new? Trends Pharmacol Sci 17 342-343 (1996).

2 Dahlén, S., 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. Proc Natl Acad Sci USA 80 1712-1716 (1983).

3 Busse, W.W. The role of leukotrienes in asthma and allergic rhinitis. Clin Exp Allergy 26 868-879 (1996).

4 Hedqvist, P., Dahlén, S., Gustafsson, L., et al. Biological profile of leukotrienes C₄ and D₄. Acta Physiol Scand 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. Clin Exp Allergy 32 1007-1012 (2002).

Öhd, J.F., Nielsen, C.K., Cambell, J., et al. Expression of the leukotriene D₄ receptor CysLT₁, COX-2, and other cell survival factors in colorectal adenocarcinomas. Gastroenterology 124 57-70 (2003).

Dahlén, S., 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. Proc Natl Acad Sci USA 80 1712-1716 (1983).

Hedqvist, P., Dahlén, S., Gustafsson, L., et al. Biological profile of leukotrienes C₄ and D₄. Acta Physiol Scand 110 331-333 (1980).

Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT₁ receptor. Nature 399 789-793 (1999).

Thivierge, M., Doty, M., Johnson, J., et al. IL-5 up-regulates cysteinyl leukotriene 1 receptor expression in HL-60 cells differentiated into eosinophils1. J Immunol 165 5221-5226 (2000).

Shirasaki, H., Kanaizumi, E., Watanabe, K., et al. Expression and localization of the cysteinyl leukotriene 1 receptor in human nasal mucosa. Clin Exp Allergy 32 1007-1012 (2002).

Gorenne, I., Norel, X., and Brink, C. Cysteinyl leukotriene receptors in the human lung: What’s new? Trends Pharmacol Sci 17 342-343 (1996).

Busse, W.W. The role of leukotrienes in asthma and allergic rhinitis. Clin Exp Allergy 26 868-879 (1996).

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