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Item No. 120550
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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
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2. 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(6), 1712-1716 (1983).
3. The role of leukotrienes in asthma and allergic rhinitis. Clin. Exp. Allergy 26(8), 868-879 (1996).
4. Biological profile of leukotrienes C4 and D4. Acta Physiol. Scand. 110(3), 331-333 (1980).
5. Characterization of the human cysteinyl leukotriene 2 receptor. The Journal of Biological Chemisty 275(39), 30531-30536 (2000).
6. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399(6738), 789-793 (1999).
7. The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT2 receptor. Biochem. Biophys. Res. Commun. 274, 316-322 (2000).