Biological Activity
BX430 is a selective noncompetitive allosteric antagonist of human P2X4 receptor channels. P2X4 receptors are highly expressed in the CNS, and have been studied as a therapeutic target for neuropathic pain and inflammation, and treatment of traumatic brain injury, cerebral ischemia, and spinal cord injury. BX430 is highly selective for human P2X4, with minimal activity towards other P2X subtypes, including P2X1–P2X3, P2X5, and P2X7. BX430 is also an antagonist of zebrafish P2X4 but has no effect on r at and mouse P2X4 receptors. BX430 has an IC50 value of 540 nM.
