MRS4719

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[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

Research Areas >> Neurological Disease

IC50: 0.503 μM (P2X4 receptor)[1]

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[1].

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[1]. 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)[1] 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)[1] 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)[1] 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.