A non-selective COX inhibitor
6-methoxy Naphthalene Acetic Acid is a competitive and non-selective COX inhibitor with Ki values of 21 and 19 μM for ovine COX-1 and -2, respectively [1][2][3].
Cyclooxygenase (COX), also known as prostaglandin-endoperoxide synthase (PTGS, PGHS), is an enzyme responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. COX-1 is the constitutive isoform and is mainly responsible for the synthesis of cytoprotective prostaglandins in the gastrointestinal tract (GI) and of the proaggregatory thromboxane in blood platelets. COX-2 is inducible and short-lived that is stimulated by endotoxin, cytokines, and mitogens. COX-2 plays important roles in prostaglandin biosynthesis in inflammatory cells the central nervous system [1][2].
6-methoxy Naphthalene Acetic Acid (6-MNA) is a competitive and non-selective COX inhibitor with Ki values of 21 and 19 μM for ovine COX-1 and -2, respectively [1][2]. 6-MNA is a metabolite of nebumetome. 6-MNA inhibited human recombinant COX-1 and -2 with IC50 values of 70 and 20 μM, respectively [1].
参考文献:
[1].? Barnett J, Chow J, Ives D, et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochim Biophys Acta. 1994 Nov 16;1209(1):130-9.
[2].? Johnson JL, Wimsatt J, Buckel SD, et al. Purification and characterization of prostaglandin H synthase-2 from sheep placental cotyledons. Arch Biochem Biophys. 1995 Dec 1;324(1):26-34.
[3].? Laneuville O1, Breuer DK, Dewitt DL, et al. Differential inhibition of human prostaglandin endoperoxide H synthases-1 and -2 by nonsteroidal anti-inflammatory drugs. J Pharmacol Exp Ther. 1994 Nov;271(2):927-34.
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