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Prostaglandin G/H synthase 2 Prostaglandin E synthase Prostacyclin synthase Thromboxane-A synthase Cytosolic phospholipase A2 Prostaglandin G/H synthase 1 Prostaglandin G/H synthase 1 Celecoxib Celecoxib Prostaglandin H2 Prostaglandin E2 Prostaglandin I2 Thromboxane A2 Arachidonic acid O2 Prostaglandin G2 H2O Heme Glutathione Heme Heme Phospholipids Acceptor Reduced acceptor Prostaglandin G/H synthase 2 Heme Heme Heme Calcium Endoplasmic Reticulum Cytosol Extracellular space Celcoxib inhibits COX-2 (prostaglandin G/H synthase 2) on the endoplasmic reticulum membrane, preventing the conversion of arachidonic acid into PGH2. Prostaglandin H2 synthesis is reduced COX-1 synthesizes prostaglandins necessary for normal gastrointestinal and renal function. COX-2 is responsible for prostaglandin synthesis during tissue injury and inflammation. Inhibition of COX-2 provides anti-inflammatory activity. Prostaglandin E2 is responsible for inflammation and pain by activating immune cells and stimulating pain fibres. Lower concentrations of prostaglandin E2 lowers inflammatory and pain response, hence an analgesic effect is seen. Decreasing PGE2 in the central nervous system also has an antipyretic effect. Inflamed Human Cell
Endoplasmic Reticulum PTGS2 PTGES PTGIS TBXAS1 PLA2G4A PTGS1 PTGS1 Celecoxib Celecoxib Prostaglandin H2 Prostaglandin E2 Prostaglandin I2 Thromboxane A2 Arachidonic acid Oxygen Prostaglandin G2 Water Phospholipids Acceptor Reduced acceptor PTGS2
PTGS2 PTGES PTGIS TBXAS1 PLA2G4A PTGS1 PTGS1 Celcoxb Celcoxb PGH2 PGE2 PrstgI2 ThrmbA2 20:4 O2 PGG2 H2O Heme GSH Heme Heme Phosp Accepto RA PTGS2 Heme Heme Heme Ca2+ Endoplasmic Reticulum Cytosol Extracellular space Celcoxib inhibits COX-2 (prostaglandin G/H synthase 2) on the endoplasmic reticulum membrane, preventing the conversion of arachidonic acid into PGH2. Prostaglandin H2 synthesis is reduced COX-1 synthesizes prostaglandins necessary for normal gastrointestinal and renal function. COX-2 is responsible for prostaglandin synthesis during tissue injury and inflammation. Inhibition of COX-2 provides anti-inflammatory activity. Prostaglandin E2 is responsible for inflammation and pain by activating immune cells and stimulating pain fibres. Lower concentrations of prostaglandin E2 lowers inflammatory and pain response, hence an analgesic effect is seen. Decreasing PGE2 in the central nervous system also has an antipyretic effect. Inflamed Human Cell
Endoplasmic Reticulum PTGS2 PTGES PTGIS TBXAS1 PLA2G4A PTGS1 PTGS1 Celcoxb Celcoxb PGH2 PGE2 PrstgI2 ThrmbA2 20:4 O2 PGG2 H2O Phosp Accepto RA PTGS2