| Description | Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia. |
| In vivo | 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 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 increases monocyte chemoattractant protein-1 and interleukin-8 mRNA expression in the whole lung of guinea pigs. 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 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. 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. |
| Target activity | TXA2 synthase:11 nM |
| Synonyms | 奥扎格雷, OKY-046, Domenan |
| molecular weight | 228.25 |
| Molecular formula | C13H12N2O2 |
| CAS | 82571-53-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 2.28 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Ishitsuka Y, et al. J Pharmacol Sci, 2009, 111(2), 211-215. 2. Imamura T, et al. Arzneimittelforschung, 2003, 53(10), 688-694. 3. Ichikawa K, et al. Pharmacology, 1999, 59(5), 257-265. 4. Ishitsuka Y, et al. J Pharm Pharmacol, 2004, 56(4), 513-520. 5. Naito J, et al. Eur J Pharmacol. 1983, 91(1), 41-48. |