AA-861 is an inhibitor of 5-lipoxygenase (5-LO; IC50 = 0.8 ?M).1 It is greater than 100-fold selective for 5-LO over 12-LO and cyclooxygenase (COX). AA-861 inhibits the production of 5-HETE and leukotriene B4 induced by A23187 with IC50 values of 0.03 and 0.08 ?M, respectively, in isolated rat peritoneal macrophages.2 It reduces paw edema, pleurisy, and cell infiltration induced by carrageenan in rats when administered at a dose of 80 mg/kg. AA-861 (20 mg/kg) reduces ovalbumin-induced bronchoconstriction in an ovalbumin-sensitized guinea pig model of experimental allergic asthma.
1.Yoshimoto, T., Yokoyama, C., Ochi, K., et al.2,3,5-Trimethyl-6-(12-hydroxy-5,10-dodecadiynyl)-l,4-benzoquinone (AA861), a selective inhibitor of the 5-lipoxygenase reaction and the biosynthesis of slow-reacting substance of anaphylaxisBiochim. Biophys. Acta713(2)470-473(1982) 2.Ashida, Y., Saijo, T., Kuriki, H., et al.Pharmacological profile of AA-861, a 5-lipoxygenase inhibitorProstaglandins26(6)955-972(1983)