ArticleBritish journal of pharmacology2004
Chelerythrine and other benzophenanthridine alkaloids block the human P2X7 receptor.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 49 citations in OpenAlex.
- ComTarget: Small-Molecule Target Prediction with Combinatorial Modeling.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Screening herbal and natural product libraries to aid discovery of novel allosteric modulators of human P2X7.Purinergic signalling · 2025Article
- Role and therapeutic targets of P2X7 receptors in neurodegenerative diseases.Frontiers in immunology · 2024Review
- Rediscovery of Traditional Plant Medicine: An Underestimated Anticancer Drug of Chelerythrine.Frontiers in pharmacology · 2022Review
- P2XFrontiers in cellular neuroscience · 2021Review
- P2RX7 Purinoceptor as a Therapeutic Target-The Second Coming?Frontiers in chemistry · 2018Review
- Chelerythrine Attenuates the Inflammation of Lipopolysaccharide-Induced Acute Lung Inflammation Through NF-κB Signaling Pathway Mediated by Nrf2.Frontiers in pharmacology · 2018Article
- Sanguinaria canadensis: Traditional Medicine, Phytochemical Composition, Biological Activities and Current Uses.International journal of molecular sciences · 2016Review
- Paroxetine suppresses recombinant human P2X7 responses.Purinergic signalling · 2015Article
- Rhein antagonizes P2X7 receptor in rat peritoneal macrophages.Scientific reports · 2015Article
- Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism.PloS one · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels.British journal of pharmacology · 2013Article
- Physiological roles and potential therapeutic applications of the P2X7 receptor in inflammation and pain.Molecules (Basel, Switzerland) · 2013Review
- P2X7 receptor activation induces reactive oxygen species formation in erythroid cells.Purinergic signalling · 2013Article
- Article
- Action of natural products on p2 receptors: a reinvented era for drug discovery.Molecules (Basel, Switzerland) · 2012Review
- The anti-invasive activity of synthetic alkaloid ethoxyfagaronine on L1210 leukemia cells is mediated by down-regulation of plasminogen activators and MT1-MMP expression and activity.Investigational new drugs · 2011Article
- Large-conductance channel formation mediated by P2X7 receptor activation is regulated through distinct intracellular signaling pathways in peritoneal macrophages and 2BH4 cells.Naunyn-Schmiedeberg's archives of pharmacology · 2010Article
- P2X(7) receptor: Death or life?Purinergic signalling · 2005Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1 Extracellular ATP can activate a cation-selective channel/pore on human B-lymphocytes, known as the P2X7 receptor. Activation of this receptor is linked to PLD stimulation. We have used ATP-induced 86Rb+ (K+) efflux to examine the effect of benzophenanthridine alkaloids on P2X7 channel/pore function in human B-lymphocytes. 2 Both ATP and the nucleotide analogue 2'-3'-O-(4-benzoylbenzoyl)-ATP (BzATP) induced an 86Rb+ efflux, which was completely inhibited by the isoquinoline derivative 1-(N,O-bis[5-isoquinolinesulphonyl]-N-methyl-l-tyrosyl)-4-phenylpiperazine (KN-62), a potent P2X7 receptor antagonist. 3 The benzophenanthridine alkaloid chelerythrine, a potent PKC inhibitor, inhibited the ATP-induced 86Rb+ efflux by 73.4+/-3.5% and with an IC50 of 5.6+/-2.3 microm. Similarly, other members of this family of compounds, sanguinarine and berberine, blocked the ATP-induced 86Rb+ efflux by 58.8+/-4.8 and 61.1+/-8.0%, respectively. 4 Concentration-effect curves to ATP estimated an EC50 value of 78 microm and in the presence of 5 and 10 microm chelerythrine this increased slightly to 110 and 150 microm, respectively, which fits a noncompetitive inhibitor profile for chelerythrine. 5 Chelerythrine at 10 microm was effective at inhibiting the ATP-induced PLD stimulation in B-lymphocytes by 94.2+/-21.9% and the phorbol 12-myristate 13-acetate-induced PLD stimulation by 68.2+/-7.4%. 6 This study demonstrates that chelerythrine in addition to PKC inhibition has a noncompetitive inhibitory action on the P2X7 receptor itself.
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