P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC 50 s of 25 nM, 92 nM and 126 nM for human P2X3 , rat P2X3 and guinea pig P2X3 receptors , respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.
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