104869-31-0

104869-31-0 structure

Name: NF023
Chemical Name: sodium,8-[[3-[[3-[(4,6,8-trisulfonaphthalen-1-yl)carbamoyl]phenyl]carbamoylamino]benzoyl]amino]naphthalene-1,3,5-trisulfonic acid
CAS Number: 104869-31-0
Molecular Formula: C₃₅H₂₀N₄Na₆O₂₁S₆
Molecular Weight: 1162.88000
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
Create Date: 2017-03-17 11:10:37
Modify Date: 2024-01-16 19:46:47
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].

Name	sodium,8-[[3-[[3-[(4,6,8-trisulfonaphthalen-1-yl)carbamoyl]phenyl]carbamoylamino]benzoyl]amino]naphthalene-1,3,5-trisulfonic acid
Synonyms	NF 023 ML 786 dihydrochloride

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.