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MK-571 is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (Ki = 2.1 nM in a radioligand binding assay using isolated human lung membranes).1 It inhibits contractions induced by leukotriene D4 (LTD4; Item No. 20310) or LTE4 (Item No. 20410) in histamine-primed isolated guinea pig trachea (pA2s = 9.4 and 9.1, respectively), but does not inhibit contractions induced by LTC4 (Item No. 20210) in histamine-primed isolated guinea pig trachea when used at a concentration of 190 nM. MK-571 (100 nM) inhibits LTD4-induced calcium mobilization in COS-7 monkey kidney cells expressing the human CysLT1 receptor in a reporter assay.2 MK-571 (5 mg/kg) improves tissue damping and elasticity, markers of lung function, and decreases IL-4 and IL-5 levels in bronchoalveolar lavage fluid (BALF) in a mouse model of ovalbumin-induced asthma.3
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1. Pharmacology of L-
2. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399(6738), 789-793 (1999).
3. Cysteinyl leukotriene induces eosinophil extracellular trap formation via cysteinyl leukotriene 1 receptor in a murine model of asthma. Exp. Lung Res. 47(8), 355-367 (2021).
Cysteinyl leukotriene induces eosinophil extracellular trap formation via cysteinyl leukotriene 1 receptor in a murine model of asthma. Exp. Lung Res. 47(8), 355-367 (2021).
P2Y6 signaling in alveolar macrophages prevents leukotriene-
Selectivity of recombinant human leukotriene D4, leukotriene B4, and lipoxin A4 receptors with aspirin-