MRS4719 is a potent P2X4 receptor antagonist with an IC 50 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 [Ca 2+ ] i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.