Azapropazone

Azapropazone is an orally active nonsteroidal anti-inflammatory agent. Azapropazone inhibits Xanthine oxidase activity with an IC₅₀ of 70-140 μg/mL. Azapropazone exerts significant cardiomyocyte protective effects on dogs with ischemia-reperfusion injury. Azapropazone reduces arthritis. Azapropazone inhibits Adrenaline-induced platelet aggregation. Azapropazone can be used for the research of myocardial ischemia and reperfusion injury, adjuvant arthritis, and gouty arthritis^[1][2][3]. In Vitro:Azapropazone (70-140 μg/mL) inhibits xanthine oxidase activity in vitro with an IC₅₀ of 70-140 μg/mL^[1].
Azapropazone (40-400 μg/mL) inhibits multiple neutrophil functions (migration, aggregation)^[1].
Azapropazone (10-200 μM; 10 min) potently inhibits superoxide anion generation by human PMNs stimulated with polyhistidine or TPA (half-maximal inhibition at ~15 μM) but not by histone-coated streptococci with cytochalasin B^[2].
Azapropazone (5 μM; 1-5 min before or concurrent with stimulus addition) inhibits adrenaline-induced human platelet aggregation but has no effect on ADP- or thrombin-induced aggregation^[2]. In Vivo:Azapropazone (50-100 mg/kg; i.v.; 30 minutes before vascular occlusion, 5 minutes before vascular occlusion release, and 2.5 hours after vascular occlusion release) exerts significant cardiomyocyte protective effects on dogs with ischemia-reperfusion injury. It reduces the degree and scope of ischemia, limits the infarct size in myocardial regions with mild to moderate blood flow restriction, and has no effect on regions with severe blood flow restriction^[1].
Azapropazone (150-200 mg/kg; p.o.; 10-14 days) significantly reduces joint swelling, cartilage damage and clinical disease activity in rats with established adjuvant-induced arthritis^[2].