Biochem/physiol Actions

Standard NSAID and cyclooxygenase (COX) inhibitor. Major metabolites are 4´-hydroxydiclofenac and 5´-hydroxydiclofenac. Has been used as substrate selective for CYP2C9.

Diclofenac sodium salt is a nonsteroidal anti-inflammatory drug (NSAID) that acts as a competitive and irreversible inhibitor of prostaglandin synthetase. Its analgesic and anti-inflammatory activities are based on the prevention of the synthesis of arachinodate metabolites via cyclooxygenase inhibition. It is found to hinder the conversion of arachidonic acid to prostaglandins, which mediate inflammatory process. The NSAIDs are found to inhibit both cyclooxygenase enzymes, COX-1 and COX-2, causing undesirable gastrointestinal effect. Diclofenac sodium also functions as a scavenger of free radicals and serves a radioprotective role in restoring supercoiled form of plasmid DNA damaged by radiation back to normal. Diclofenac sodium is oxidized by the donation of electron and transfer of hydrogen atom. It can be a potential radioprotective agent.

Application

Diclofenac sodium has been used:
? to investigate its radioprotective potential in a study
? to determine the basic viscosity and hydrodynamic values of the solubilizers and their micellar adducts in a study
? as a standard for potentiometric and fluorimetric determination of diclofenac in a sequential injection analysis system
? to inhibit phase II drug metabolizing enzyme (DME) in a study to investigate the inhibitory effects of an ethanol extract of Descurainia sophia seeds on Phase I and II DMEs

Features and Benefits

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This compound is featured on the Acid-Sensing (Proton-gated) Ion Channels (ASICs) and Nuclear Receptors (PPARs) pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

法律信息

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