| In Vitro | In vitro activity: NXY-059 is more soluble than the spin trapping agent α-phenyl-N-tert-butyl nitrone (PBN). In an in vitro blood-brain barrier (BBB) model, 250 mM of NXY-059 administered at the onset or up to 4 h after oxygen glucose deprivation (OGD) produces a significant reduction in the increased BBB permeability caused by OGD. Furthermore, OGD produces a huge influx of tissue plasminogen activator across the BBB, which is substantially reduced by NXY-059. |
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| In Vivo | NXY-059 reduces infarct volume in rats subjected to 2 hours of middle cerebral artery occlusion in a dose-dependent manner. At equimolar doses (3.0 mg/kg for NXY-059 and 1.4 mg/kg for PBN), NXY-059 is more efficacious than PBN. Similar results are obtained when a recovery period of 7 days is allowed. The window of therapeutic opportunity for NXY-059 is 3 to 6 hours after the start of recirculation. NXY-059, a free radical-trapping agent, has a substantial protective effect, lessening the disability caused by an experimentally induced stroke in a primate species. NXY-059 treatment reduces the overall amount of brain damage by>50% of saline-treatment values, with similar levels of protection afforded to both white and gray matter. Treatment with NXY-059 (50 mg/kg subcutaneous plus 8.8 mg/kg/h for 3 days subcutaneous delivered via implanted osmotic pumps) significantly decreases neurological impairment following intracerebral hemorrhage in rat, and reduces the neutrophil infiltrate observed 48 hours post-hemorrhage in the vicinity of the hematoma, and the number of TUNEL-positive cells 48 hours post-hemorrhage at the hematoma margin. |
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| Animal model | Monofilament fishing line is used to produce occlusion and neurologic deficit in male Wistar rats |
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| Formulation & Dosage | Dissolved in physiological saline; 0.3, 3.0 or 30 mg/kg; Injected via the right jugular vein |
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| References | J Cereb Blood Flow Metab. 1999 Jul;19(7):778-87; Stroke. 2001 Jan;32(1):190-8; Brain Res. 2009 Oct 19;1294:144-52. |
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