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^[4].

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)^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . F Soto, et al. Antagonistic Properties of the Suramin Analogue NF023 at Heterologously Expressed P2X Receptors. Neuropharmacology. 1999 Jan;38(1):141-9.  [Content Brief]

  . M Freissmuth, et al. Suramin Analogues as Subtype-Selective G Protein Inhibitors. Mol Pharmacol. 1996 Apr;49(4):602-11.  [Content Brief]

  . G Lambrecht, et al. Agonists and Antagonists Acting at P2X Receptors: Selectivity Profiles and Functional Implications. Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):340-50.  [Content Brief]

  [4]. M Silva-Ramos, et al. Activation of Prejunctional P2x2/3 Heterotrimers by ATP Enhances the Cholinergic Tone in Obstructed Human Urinary Bladders. J Pharmacol Exp Ther. 2020 Jan;372(1):63-72.  [Content Brief]