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Differential inhibition of COX-1 and COX-2 by NSAIDs: a summary of results obtained using various test systems

  • M. Pairet
  • J. Van Ryn
  • A. Mauz
  • H. Schierok
  • W. Diederen
  • D. Türck
  • G. Engelhardt

Abstract

Since the discovery of a second isoenzyme of cyclooxygenase (COX), COX-21,2, it has been hypothesized that the anti-inflammatory effects of non-steroid anti-inflammatory drugs (NSAIDs) are achieved through a mechanism different from that underlying the often seen side-effects of these compounds, including disruption of cytoprotection of the stomach, toxic effects on the kidney and inhibition of platelet aggregation3. COX-1 is the constitutive isozyme found under physiological conditions in most tissues, a so-called ‘housekeeping’ enzyme, while COX-2 expression is induced, particularly during inflammatory processes4. It has been proposed that COX-2 inhibition is the relevant target for the anti-inflammatory effects of NSAIDs, whereas inhibition of COX-1 is responsible for their gastric and renal side-effects3,4. Most available NSAIDs block both COX-1 and COX-2 to a similar degree; however, newer compounds with selective inhibition of COX-2 should retain the anti-inflammatory activity of NSAIDs but have minimal gastro-intestinal side-effects.

Keywords

Differential Inhibition Blood Assay Standard NSAID Sodium Naproxen Human Recombinant Enzyme 
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Copyright information

© Springer Science+Business Media Dordrecht 1998

Authors and Affiliations

  • M. Pairet
  • J. Van Ryn
  • A. Mauz
  • H. Schierok
  • W. Diederen
  • D. Türck
  • G. Engelhardt

There are no affiliations available

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