SB 290157

A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM; does not antagonize the C5aR or 5 other chemotactic GPCRs on human neutrophils; blocks C3a-induced C3aR internalization and C3a-induced Ca(2+) mobilization in RBL-C3aR cells and human neutrophils with IC50 of 27.7 and 28 nM, respectively; also inhibits C3a-induced Ca2+ mobilization of mouse and guinea pig C3aRS with IC50 of 7 and 12.5 nM, respectively; potently inhibits C3a-mediated ATP release from guinea pig platelets and inhibits C3a-induced potentiation of the contractile response to field stimulation of perfused rat caudal artery, demonstrates antiinflammatory activity in animal models.

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