A novel, potent, orally bioavailable antagonist of P2X3/P2X2/3 receptors (pIC50 = 8 in human and rat; pIC50 = 7.3 for human P2X2/3 receptor). Shown to be highly brain penetrant with a brain to plasma ratio of 6. Blocks agonist-evoked intracellular Ca2+ flux and inward currents in nanomolar range (10nM to 1uM) in cell lines recombinantly expressing human P2X3 and P2X2/3 receptors. Exhibits desirable pharmacokinetic properties (t1/2 = 1.63 h and Tmax = 30 min).
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