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编 号:F756301
分子式:C26H13N5O3S.C6H15N
分子量:504.6
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生物活性:
MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.

体内研究:
MRS4719 (compound 21u) (0.5-3 mg/kg; 3 days continuous infusion with an Alzet minipump) reduce infarct volume and reduced brain atrophy; does not improve motor coordination and balance as assessed using rotarod; improves learning and memory after stroke.Animal Model:Male and female young C57B/6 mice (8-12 weeks; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)
Dosage:0.5, 1.5 and 3 mg/kg
Administration:3 days continuous infusion with an Alzet minipump
Result:Caused significant neuroprotection using total hemispheric infarct volume size at doses 1.5 and 3.0 mg/kg.
Animal Model:Middle-aged C57B/6 mice (11-12 month-old; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)
Dosage:1.5 and 3 mg/kg
Administration:3 days continuous infusion with an Alzet minipump
Result:Did not improve motor coordination and balance as assessed using rotarod.
Animal Model:Middle-aged C57B/6 mice (11-12 month-old; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)
Dosage:3 mg/kg
Administration:3 days continuous infusion with an Alzet minipump
Result:Improved dose-dependently learning and memory after stroke and reached statistical significance at a dose of 3 mg/kg.

体外研究:
MRS4719 (compound 21u) (0.1, 0.3, 0.6, 1.0 and 3.0 μM; 15 min) inhibits P2X4R-mediated Ca2+ influx in human subjects.
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