COX-2 inhibition and the control of pain.
The discovery of the two isoenzymes of cyclooxygenase COX-1 and COX-2 and their separate functions, localization and regulation, has initiated the search for new and more selective inhibitors of prostaglandin biosynthesis. Selective COX-2 inhibitors were developed in order to improve an anti-inflammatory and analgesic specificity and potency. The role of inducible COX-2 at the peripheral site of inflammation is well known. The discovery of COX-2 in the spinal cord suggests that it is responsible for spinal prostaglandin release in nociceptive processes following a peripheral inflammatory stimulus. In the future, selective COX-2 inhibitors such as celecoxib (GD Searle & Co), rofecoxib (Merck & Co Inc) and the recently developed etoricoxib (Merck & Co Inc) may play an important role in the treatment of a wider range of pain conditions in addition to their present use as anti-inflammatory and analgesic drugs.
Kiefer
Werner
W
Department of Chemistry and Pharmacy, Johannes Gutenberg-University, Institute of Pharmacy, Staudinger Weg 5, D-55099 Mainz, Germany. dannhardt@mail.uni-mainz.de
Dannhardt
Gerd
G
D000818:Animals; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008565:Membrane Proteins; D010146:Pain / Q000188:drug therapy* / Q000201:enzymology*; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases