Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity.

Article Details

Citation

Chambers RJ, Marfat A, Antognoli GW, Cheng JB, Damon DB, Kuperman AV, Liston TC, Mebus C, Pillar JS, Shirley JT, Watson JW

Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity.

Bioorg Med Chem Lett. 1999 Sep 20;9(18):2773-8.

PubMed ID
10509933 [ View in PubMed
]
Abstract

CP-199,330 (3) and CP-199,331 (4) are cysLT1 receptor antagonists that are equipotent to marketed cysLT1 receptor antagonists zafirlukast and pranlukast, show good pharmacokinetics in rats and monkeys, and are devoid of liver toxicity in monkeys as seen in CP-85,958 (1).

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ZafirlukastCysteinyl leukotriene receptor 1Ki (nM)2N/AN/ADetails