Cat. No. 1240
Chemical Name: 8,8'-[carbonylbis(imino-3,1-phenylen
Biological ActivityA subtype-selective, competitive and reversible P2X1 receptor antagonist. Displays IC50 values of 0.21, 28.9, > 50 and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively. Selective over adrenoceptors, histamine and P2Y receptors. Also selectively inhibits the α-subunit of Go/i (EC50 ~300 nM).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Sneddon et al (2000) The effect of P2 receptor antagonists and ATPase inhibition on sympathetic purinergic neurotransmission in the guinea-pig isolated vas deferens. Br.J.Pharmacol. 129 1089. PMID: 10725256.
Soto et al (1999) Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors. Neuropharmacology 38 141. PMID: 10193905.
Freissmuth et al (1996) Suramin analogues as subtype-selective G protein inhibitors. Mol.Pharmacol. 49 602. PMID: 8609887.
Van Rhee et al (1994) Novel competitive antagonists for P2 purinoceptors. Eur.J.Pharmacol. 268 1. PMID: 7925607.
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Citations are publications that use Tocris products. Selected citations for NF 023 include:
Ren et al (2014) The approved pediatric drug suramin identified as a clinical candidate for the treatment of EV71 infection-suramin inhibits EV71 infection in vitro and in vivo. Emerg Microbes Infect 3 e62. PMID: 26038755.
Beckham et al (2013) Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling. Oncogenesis 2 e49. PMID: 23732709.
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787. PMID: 22753954.
Donnelly-Roberts et al (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br J Pharmacol 157 1203. PMID: 19558545.
Labrakakis et al (2003) Localization and function of ATP and GABAA receptors expressed by nociceptors and other postnatal sensory neurons in rat. J Physiol 549 131. PMID: 12665615.
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Keywords: NF 023, supplier, inhibitors, inhibits, Go/i, α-subunits, alpha-subunits, P2X, purinoceptors, antagonists, Selective, competitive, G-Protein, Signaling, Signalling, Heterotrimeric, Receptors, Purinergic, NF023, Tocris Bioscience, Purinergic (P2X) Receptor Antagonist products