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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]. | [in vivo]
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. |
| [References]
[1] Toti KS, et al. Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-diones as P2X4 Receptor Antagonists. J Med Chem. 2022 Sep 23. DOI:10.1021/acs.jmedchem.2c01197 |
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