Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain

Karen Seibert, Yan Zhang, Kathleen Leahy, Scott Hauser, Jaime Masferrer, William Perkins, Len Lee, Peter Isakson

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1452 Scopus citations


Nonsteroidal antiinflammatory drugs (NSAIDs) are widely used for the treatment of inflammatory diseases, but significant side effects such as gastrointestinal erosion and renal damage limit their use. NSAIDs inhibit the enzyme cyclooxygenase (COX), which catalyzes the conversion of arachidonic acid to prostaglandins (PGs) and thromboxane. Two forms of COX have been identified-COX-1, which is constitutively expressed in most tissues and organs, and the inducible enzyme, COX-2, which has been localized primarily to inflammatory cells and tissues. In an animal model of acute inflammation (injection of carrageenan into the footpad), edema was produced that was associated with marked accumulation of COX-2 mRNA and thromboxane. A selective inhibitor of COX-2 (SC-58125) inhibited edema at the inflammatory site and was analgesic but had no effect on PG production in the stomach and did not cause gastric toxicity. These data suggest that selective inhibition of COX-2 may produce superior antiinflammatory drugs with substantial safety advantages over existing NSAIDs.

Original languageEnglish
Pages (from-to)12013-12017
Number of pages5
JournalProceedings of the National Academy of Sciences of the United States of America
Issue number25
StatePublished - Dec 6 1994


  • hyperalgesia
  • nonsteroidal antiinflammatory drug
  • prostaglandin


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