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Description

A tetrahydronaphthalenyl carboxamide compound that acts as a potent, specific and orally active C5a receptor antagonist. Shown to inhibit the binding of 125I-rhC5a to human neutrophils with a Ki of 2.2 nM, as well as C5a-induced intracellular Ca2+-mobilization, chemotaxis and reactive oxygen species (ROS) generation (IC50 = 3.1 nM, 2.7 nM and 1.6 nM, respectively) with no agonist activity up to 10 µ,M. Shown to prevent C5a-induced neutrophenia in gerbils (100 µ,g/kg i.v. or 3-30 mg/kg orally)., A potent, specific, and orally active C5a receptor antagonist. Shown to inhibit the binding of 125I-rhC5a to human neutrophils with a Ki of 2.2 nM, as well as C5a-induced intracellular Ca2+-mobilization, chemotaxis and reactive oxygen species (ROS) generation (IC50 = 3.1 nM, 2.7 nM and 1.6 nM, respectively) with no agonist activity up to 10 µ,M. Shown to prevent C5a-induced neutrophenia in gerbils (100 µ,g/kg i.v. or 3-30 mg/kg orally).