NF023

Names

[ Name ]:
NF023

[Synonym ]:
NF 023
ML 786 dihydrochloride

Biological Activity

[Description]:

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[1][2][3][4].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

Research Areas >> Neurological Disease

[In Vitro]

NF023 is selective for recombinant Gi alpha-1 and recombinant Go alpha (EC50 value of approximately 300 nM)[2]. 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 (KB=1.190.2 μM)[4].

[In Vivo]

NF023 (100 µmol/kg i.v.) antagonizes vasopressor responses to α,β-mATP but not to noradrenaline In pithed rats[3].

[References]

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

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

[3]. 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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₅H₂₀N₄Na₆O₂₁S₆

[ Molecular Weight ]:
1162.88000

[ Exact Mass ]:
1161.83000

[ PSA ]:
492.81000

[ LogP ]:
8.34300

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
S26

Related Compounds

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