PSFL2915 is a selective inhibitor of the P2X receptor family, exhibiting an IC50 of 0.319 μM for human P2X3 and 0.261 μM for rat P2X2/3, with approximately 42-fold selectivity for human P2X3 over human P2X2. This compound inhibits human P2X3 activation by disrupting the allosteric tightening of the inner pocket necessary for channel opening, with dependency on magnesium for its inhibitory effect. Additionally, PSFL2915 demonstrates inhibitory activity against rat P2X2/3 and human P2X2 receptors, while showing minimal effects on human P2X1, P2X4, and P2X7 receptors. It is applicable in chronic cough research.
PSFL2915 is a selective inhibitor of the P2X receptor family, exhibiting an IC50 of 0.319 μM for human P2X3 and 0.261 μM for rat P2X2/3, with approximately 42-fold selectivity for human P2X3 over human P2X2. This compound inhibits human P2X3 activation by disrupting the allosteric tightening of the inner pocket necessary for channel opening, with dependency on magnesium for its inhibitory effect. Additionally, PSFL2915 demonstrates inhibitory activity against rat P2X2/3 and human P2X2 receptors, while showing minimal effects on human P2X1, P2X4, and P2X7 receptors. It is applicable in chronic cough research.
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