SKF-86002

SKF 86002 is an anti-inflammatory agent.^1,2,3,4 It inhibits rat seminal vesicle prostaglandin H₂ (PGH₂) synthase (IC₅₀ = 120 ?M), as well as prostanoid production by rat basophilic leukemia (RBL-1) cells and human monocytes (IC₅₀s = 70 and 1 ?M, respectively).¹ SKF 86002 inhibits leukotriene B₄ (LTB₄) and LTC₄ production induced by A23187 in human neutrophils and monocytes, respectively (IC₅₀ = 20 ?M for both). It also inhibits LPS-induced IL-1 production in human monocytes (IC₅₀ = 1.3 ?M).² SKF 86002 (10, 30, and 90 mg/kg) reduces hindleg volume in rat models of adjuvant- or collagen-induced arthritis.³ It also decreases serum levels of TNF-α and increases survival in a mouse model of LPS and galactosamine-induced endotoxic shock when administered at a dose of 100 mg/kg.⁴

1.Griswold, D.E., Marshall, P.J., Webb, E.F., et al.SK&F 86002: A structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acidBiochem. Pharmacol.36(20)3463-3470(1987) 2.Lee, J.C., Griswold, D.E., Votta, B., et al.Inhibition of monocyte IL-1 production by the anti-inflammatory compound, SK&F 86002Int. J. Immunopharmacol.10(7)835-843(1988) 3.DiMartino, M.J., Griswold, D.E., Berkowitz, B.A., et al.Pharmacologic characterization of the antiinflammatory properties of a new dual inhibitor of lipoxygenase and cyclooxygenaseAgents Actions20(1-2)113-123(1987) 4.Badger, A.M., Olivera, D., Talmadge, J.E., et al.Protective effect of SK&F 86002, a novel dual inhibitor of arachidonic acid metabolism, in murine models of endotoxin shock: Inhibition of tumor necrosis factor as a possible mechanism of actionCirc. Shock27(1)51-61(1989)