A 5-LO inhibitor
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)
Animal experiment: | Rats[3]Pancreatitis is induced in rats by retrograde injection of 0.4 mL/kg body wt of 6% taurocholic acid into the pancreatic duct. The animals are divided into three groups: control group; administered Docebenone in a single dose of 30 mg/kg; and administered Docebenone in a single dose of 60 mg/kg. The following parameters are examined: serum amylase, lipase, trypsin, blood sugar, and survival rate[3]. |
参考文献: [1]. Nam YH, et al. Leukotriene B(4) receptors BLT1 and BLT2 are involved in interleukin-8 production in human neutrophils induced by Trichomonas vaginalis-derived secretory products. Inflamm Res. 2012 Feb;61(2):97-102. | |
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