MK-571

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Background

MK-571 (L-660,711) is a novel potent and selective antagonist of leukotriene D4 receptor with Ki values of 0.22 nM and 2.1 nM in guinea pig and human lung membranes, respectively [1]. MK-571 is also a specific inhibitor of the multidrug resistance protein 1 (MRP1) [2].
Leukotriene D4 (LTD4) is one of the leukotrienes and is released by basophils. LTD4 induces the contraction of smooth muscle and increases vascular permeability. Cysteinyl leukotriene receptor 1 (cysLT1 receptor, LTD4 receptor) is a G protein-coupled receptor activated by LTD4 [3].
MK-571 (L-660,711) is a potent, selective and orally active leukotriene D4 receptor antagonist. MK-571 competitively antagonized contractions of guinea pig trachea and ileum induced by LTD4 (pA2 values, 9.4 and 10.5) and LTE4 (pA2 values, 9.1 and 10.4) , and antagonized contractions of human trachea induced by LTD4 with pA2 value of 8.5 [1].
In anesthetized guinea pigs, MK-571 antagonized bronchoconstriction induced by LTC4, LTD4, and LTE4 [1]. In mice, MK-571 (1, 10, 100 mg/kg) inhibited inflammatory cell infiltration in the bronchoalveolar lavage in a dose-dependent way with maximal inhibition of 90%. MK-571 also inhibited bronchial hyperreactivity and reduced lung microvascular leakage by 22% at 10 mg/kg [3].

[1]. Jones TR, Zamboni R, Belley M, et al. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol, 1989, 67(1): 17-28.
[2]. Vellenga E, Tuyt L, Wierenga BJ, et al. Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1. Br J Pharmacol, 1999, 127(2): 441-448.
[3]. Blain JF, Sirois P. Involvement of LTD(4) in allergic pulmonary inflammation in mice: modulation by cysLT(1)antagonist MK-571. Prostaglandins Leukot Essent Fatty Acids, 2000, 62(6): 361-368.