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NF023 hexasodium is a selective and competitive P2X₁ receptor antagonist, with IC₅₀ values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X₁, P2X₃, P2X₂, and P2X₄-mediated responses respectively.

NF023 is selective for recombinant Gi alpha-1 and recombinant Go alpha (EC₅₀ value of approximately 300 nM).
NF023 inhibits P2X1 receptors in a voltage-insensitive manner. NF023 (5 and 30 μM) causes a shift of the concentration-response curve to the right without affecting the maximal response to ATP (K_B=1.190.2 μM).

NF023 (100 µmol/kg i.v.) antagonizes vasopressor responses to α,β-mATP but not to noradrenaline In pithed rats.

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