Verlukast

Description: Verlukast is an (R)-enantiomer of MK-571 and a potent and selective LTD4 receptor antagonist. Verlukast showed [3H]leukotriene D4 binding in guinea-pig (IC50 = 3.1 +/- 0.5 nM) and human (IC50 = 8.0 +/- 3.0 nM) lung homogenates and dimethyl sulfoxide differentiated U937 cell membrane preparations (IC50 = 10.7 +/- 1.6 nM) but is essentially inactive versus [3H]leukotriene C4 binding in guinea-pig lung homogenates (IC50: 19 and 33 microM). Target: Others. Smiles: CN(C)C(=O)CCSC(SCCC(O)=O)c1cccc(\C=C\c2ccc3ccc(Cl)cc3n2)c1. References: Nicoll-Griffith DA, Gupta N, Twa SP, Williams H, Trimble LA, Yergey JA. Verlukast (MK-0679) conjugation with glutathione by rat liver and kidney cytosols and excretion in the bile. Drug Metab Dispos. 1995 Oct,23(10):1085-93. PubMed PMID: 8654196.