A selective, reversible inhibitor of COX-2
N-(2-phenylethyl)-Indomethacin amide is a reversible, potent and selective COX-2 inhibitor [1].
Cyclooxygenase (COX) 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].
N-(2-phenylethyl)-Indomethacin amide (N-2PIA) is a reversible, potent and selective COX-2 inhibitor that inhibits human recombinant COX-2 and ovine COX-1 with IC50 values of 0.06 and >66 μM, respectively. It is over 1000 times less potent as an inhibitor of ovine COX-1. N-(2-phenylethyl)-Indomethacin amide is an analogous derivative of indomethacin that shows selective against COX-2 [1].
In the carageenan-induced foot pad edema assay, orally administration of N-2PIA showed anti-inflammatory activity [1].
Reference:
[1].? Kalgutkar AS, Marnett AB, Crews BC, et al. Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. J Med Chem. 2000 Jul 27;43(15):2860-70.
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