Description
A dual P2X3 and P2X2/3 receptor antagonist (IC50s = 10 and 79.4 nM, respectively); selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 (IC50 = >10 µM for all); inhibits calcium flux in CHO-K1 cells expressing the rat P2X3 receptor and in 1321N1 cells expressing the human P2X3 and P2X2/3 receptors (IC50s = 8.91, 8.71, and 38.9 nM, respectively); decreases the electrical signals in the detrusor, but not striated, muscle of the bladder in female rats