| In Vitro | In vitro activity: Ozagrel(OKY-046) is an antiplatelet agent working as a thromboxane A2
synthesis inhibitor. Ozagrel was selected as the best compound of highly selective inhibitors
of TXA2 synthase. The inhibition of TXA2 synthase by ozagrel was more
effective on human and rabbit enzymes than those of other species.
Ozagrel increased 6-keto-PGF1 alpha, one of stable metabolites of PGI2,
in various isolated cells and tissues perhaps via accumulated PG
endoperoxides resulted by the inhibition of TXA2 synthase |
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| In Vivo | Ozagrel prevents oleic acid (OA) induced thromboxane A(2) generation and subsequently increased total protein concentration and the numbers of macrophages and neutrophils in bronchoalveolar lavage fluid and increased monocyte chemoattractant protein-1 andinterleukin-8 mRNA expression in the whole lung of guinea pigs. Ozagrel (3 mg/kg) decreases both the area and volume of the cortical infarction after ischemia-reperfusion of the middle cerebral artery in rat. Ozagrel also has suppressive effects on the neurologic deficits in the microthrombosis rat model. Ozagrel improves the reduced spontaneously locomotor activity and the obstruction of motor coordination in the conscious cerebral ischemia-reperfusion mouse model. Ozagrel suppresses the decrease in specific gravity of the brain tissue induced by the occlusion-reperfusion in the conscious cerebral ischemia-reperfusion SHR model, and recovers the postischemic decrease in cortical PO(2) after middle cerebral artery occlusion-reperfusion in cats. Ozagrel also increases the level of 6-keto-PGF(1alpha), a metabolite of prostaglandin I(2) (PGI(2)), in the brain tissue after cerebral ischemia-reperfusion, and the administration of PGI(2) improves the reduced spontaneous locomotor activity in the conscious cerebral ischemia-reperfusion mouse model. Ozagrel administered intravenously 30 min before oleic acid injection prevents the decrease in Pao(2) and pulmonary vascular hyper-permeability in guinea-pigs. Ozagrel also prevents increases in lactate dehydrogenase activity, a measure of lung cell injury, TXB(2) and its weight ratio to 6-keto prostaglandin F(1alpha) in bronchoalveolar lavage fluid in guinea-pigs. |
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