Abstract.
Objective and Design: To investigate the effect of JTE-522, a selective cyclooxygenase (COX)-2 inhibitor, on prostaglandin (PG) production and COX expression in rats.¶Subjects: Male rats (4-8 weeks old) were used for in vivo experiments, while for in vitro assay, rat peritoneal macrophages were used.¶Treatment: JTE-522 (1-100mg/kg) and indomethacin (0.03-10mg/kg) were administered orally. JTE-522 and reference compounds (0.01-10 μM) were subjected to COX expression.¶Results: JTE-522 inhibited the development of carrageenin-induced paw edema and PGE2 production in inflammatory paws at a dose of 10mg/kg. On the other hand, JTE-522 (1-100 mg/kg) did not affect A23187-stimulated thromboxane B2 release from whole blood or the PGE2 level in gastric mucosa. JTE-522 did not suppress lipopolysaccharide-induced COX-2 expression in peritoneal macrophages.¶Conclusion: These results indicate that JTE-522 selectively inhibits PG production mediated by COX-2 in inflammatory tissues. JTE-522 may thus represent a novel type of anti-inflammatory drug without adverse effects on the gastrointestinal tract.
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Received 16 August 1999; returned for revision 6 October 1999; accepted by M. J. Parnham 11 November 1999.
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Wakitani, K., Tazaki, H., Matsushita, M. et al. JTE-522 selectively inhibits cyclooxygenase-2-derived prostaglandin production in inflammatory tissues. Inflamm. res. 49, 117–122 (2000). https://doi.org/10.1007/s000110050568
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DOI: https://doi.org/10.1007/s000110050568