体外研究
BX430 has virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC
50
.
BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs.
Human P2X4-expressing cells treated with thapsigargin plus BX430 shows a significant reduction in the intracellular calcium rise evoked by ATP.
BX430 (5 μM) markedly reduces the amplitude of ATP-evoked intracellular calcium responses in THP-1 cells.