Antigen: human CysLT₂ receptor C-terminal amino acids 330-346 (TKCVFPVSVWLRKETRV) · Host: rabbit · Application(s): FC, WB, and IHC · 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 CysLT₂ receptor reveals it is a 346 amino acid protein with 38% homology to the CysLT₁ receptor.^5,6 The rank order of binding for leukotrienes to the cloned receptor, as determined using a radioligand binding assay, is LTC₄ = LTD₄ >> LTE₄.⁵ The mRNA for the human CysLT₂ receptor is expressed in lung macrophages, airway smooth muscle, cardiac Purkinje cells, adrenal medulla cells, peripheral blood leukocytes, spleen, placenta, and brain.^5,7

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 Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem 275 30531-30536 (2000).

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

7 Takasaki, J., Kamohara, M., Matsumoto, M., et al. The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT₂ receptor. Biochem Biophys Res Commun 274 316-322 (2000).

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).

Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem 275 30531-30536 (2000).

Takasaki, J., Kamohara, M., Matsumoto, M., et al. The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT₂ receptor. Biochem Biophys Res Commun 274 316-322 (2000).

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

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

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

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