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BLU-5937 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25nM, 92nM and 126nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. BLU-5937 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. BLU-5937 has strong anti-tussive effect[1].

BLU-5937 (500nM) is able to block αβ-meATP-induced sensitization and firing activity of isolated primary nociceptors in rat dorsal root ganglions (DRGs), through P2X3 homotrimeric receptor antagonism. The sensitizing effect of αβ-meATP and the inhibition of BLU-5937 are reversible after washout[1].

BLU-5937 (0.3-0mg/kg, oral administration; male Dunkin Hartley guinea pigs) treatment significantly reduces the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion in a guinea pig cough model[1].BLU-5937 (3 and 30mg/kg, oral) is also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs in the guinea pig[1]. Animal Model: Male Dunkin Hartley guinea pigs[1]

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