U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1 - 10 of 10 results

Status:
First approved in 1991

Class (Stereo):
CHEMICAL (ACHIRAL)



Nabumetone is a naphthylalkanone. Is is a non-selective prostaglandin G/H synthase (a.k.a. cyclooxygenase or COX) inhibitor that acts on both prostaglandin G/H synthase 1 and 2 (COX-1 and -2). Prostaglandin G/H synthase catalyzes the conversion of arachidonic acid to prostaglandin G2 and prostaglandin G2 to prostaglandin H2. Prostaglandin H2 is the precursor to a number of prostaglandins involved in fever, pain, swelling, inflammation, and platelet aggregation. The parent compound is a prodrug that undergoes hepatic biotransformation to the active compound, 6-methoxy-2-naphthylacetic acid (6MNA). The analgesic, antipyretic and anti-inflammatory effects of NSAIDs occur as a result of decreased prostaglandin synthesis. The parent compound is a prodrug, which undergoes hepatic biotransformation to the active component, 6-methoxy-2-naphthylacetic acid (6MNA), that is a potent inhibitor of prostaglandin synthesis, most likely through binding to the COX-2 and COX-1 receptors. Nabumetone is used for acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis. Nabumetone has been developed by Beecham. It is available under numerous brand names, such as Relafen, Relifex, and Gambaran.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

6-Methoxy-2-naphthalenecarboxaldehyde is a substrate of aldehyde dehydrogenase enzymes (class I, class II and class III). It was examined as indicator of the aldehyde dehydrogenase (ALDH) activity in human tissue homogenates and accessible body fluids from patients with viral and toxic liver injuries, and tumors. As intermediate, it was used in organic synthesis of enantiomerically enriched R- and S-6-MONCH- (OH)CN and fluorescent substrates for inhibition studies relating to hypertension and vascular inflammation.