Rofecoxib is a non-steroidal anti-inflammatory drug that inhibits cyclooxygenase (COX)-2 activity with 1,000-fold selectivity over that of COX-1 (IC50s = 26 nM and > 50 µM in human osteosarcoma cells).{12018} In in vivo rodent models, rofecoxib can inhibit carrageenan-induced paw edema (ID50 = 1.5 mg/kg), carrageenan-induced paw hyperalgesia (ID50 = 1.0 mg/kg), lipopolysaccharide-induced pyresis (ID50 = 0.24 mg/kg), and adjuvant-induced arthritis (ID50 = 0.74 mg/kg/day).{12018} Despite its effectiveness against pain and inflammation, rofecoxib was removed from the market in 2004 due to concerns over its long-term cardiovascular safety.{14006,14766}
产品描述
An NSAID that inhibits COX-2 activity with 1,000-fold selectivity over that of COX-1 (IC50s = 26 nM and > 50 µM in human osteosarcoma cells); effective against pain and inflammation in various rodent models
