Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

TXA2 synthase:11 nM

Administration of 3 mg/kg Ozagrel significantly reduces the area and volume of cortical infarcts in rats following cerebral middle artery occlusion and reperfusion. Ozagrel also inhibits neural deficits in a rat model of microthrombosis and enhances deteriorated spontaneous motor activity and motor coordination in a conscious mouse model of cerebral ischemia-reperfusion. Furthermore, Ozagrel prevents the increase in lactate dehydrogenase activity in guinea pig pulmonary lavage fluid and blocks the production of thromboxane A(2) induced by oleic acid in guinea pigs, subsequently reducing the total protein concentration and the numbers of macrophages and neutrophils, as well as the expression of monocyte chemoattractant protein-1 and interleukin-8 mRNA in the entire lung. In cats, Ozagrel inhibits the reduction of brain tissue-specific gravity induced by reperfusion in the SHR model of cerebral ischemia-reperfusion and restores the decreased cortical PO(2) post-ischemia upon reperfusion. Ozagrel also increases the level of 6-keto-PGF(1alpha), a metabolite of prostacyclin I(2) (PGI(2)), in the brain tissue following ischemia-reperfusion.