Nabumetone 42924-53-8

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Molecular Weight:


228.29 Nabumetone is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.





Biological Activity

Nabumetone is a nonsteroidal anti-inflammatory prodrug. Nabumetone
itself is non-acidic and, following absorption, it undergoes extensive
first-pass Metabolism to form the main circulating active metabolite
(6-MNA) which is a much more Potent Inhibitor of preferentially COX-2.






Nabumetone displays acute anti-inflammatory activity in the
carrageenan-induced oedema model in rats and the ultraviolet-induced
erythema model in guinea-pigs. Its activity in these tests is greater
than that of aspirin but less than that of naproxen and indomethacin.


In
the cotton pellet-induced granuloma model in the rat, Nabumetone is
active and produces no signs of toxicity at doses much greater than the
lowest effective dose, unlike aspirin, naproxen or indomethacin.
Nabumetone is also active in the adjuvant-induced arthritis test in
rats. In contrast to aspirin, indomethacin and naproxen, Nabumetone is
well tolerated by the stomach of fasted rats at doses in excess of those
with anti-inflammatory activity.

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Product Categories : Neuronal Signaling > COX Inhibitor