P2X4 Receptor
P2X4 receptor is an extracellular ATP-gated trimeric cation channel that supports Ca2+-linked purinergic signaling[1]. Mechanistically, P2X4 activation in spinal microglia promotes BDNF release and NR1 phosphorylation, linking receptor upregulation after peripheral nerve injury to neuropathic pain models[2]. In nerve-injury models, induced spinal microglial P2X4 is necessary and sufficient for tactile allodynia[3]. Compared with related P2X7, P2X4 shares ATP-gated cation-channel architecture but shows disputed direct P2X4/P2X7 interaction in native systems, so isoform-selective validation remains essential[4]. For experimental applications, ivermectin acts as a positive allosteric modulator of human P2X4, while NP-1815-PX, BX430, and BAY-1797 support antagonist-based interrogation of P2X4 function[5][6][7].- P2X4 links extracellular ATP sensing to Ca2+ signaling in purinergic receptor biology.- Microglial P2X4 supports neuropathic pain modeling through BDNF-associated spinal signaling.- Selective antagonists help separate P2X4 mechanisms from related P2X receptor isoforms.
References:
- [1]. Kawate T, et al. Crystal structure of the ATP-gated P2X(4) ion channel in the closed state. Nature. 2009 Jul 30;460(7255):592-8. [Content Brief]
- [2]. Ulmann L, et al. Up-regulation of P2X4 receptors in spinal microglia after peripheral nerve injury mediates BDNF release and neuropathic pain. J Neurosci. 2008 Oct 29;28(44):11263-8. [Content Brief]
- [3]. Tsuda M, et al. P2X4 receptors induced in spinal microglia gate tactile allodynia after nerve injury. Nature. 2003 Aug 14;424(6950):778-83. [Content Brief]
- [4]. Schneider M, et al. Interaction of Purinergic P2X4 and P2X7 Receptor Subunits. Front Pharmacol. 2017 Nov 22;8:860. [Content Brief]
- [5]. Priel A, et al. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004 Mar;123(3):281-93. [Content Brief]
- [6]. Matsumura Y, et al. A novel P2X4 receptor-selective antagonist produces anti-allodynic effect in a mouse model of herpetic pain. Sci Rep. 2016 Aug 31;6:32461. [Content Brief]
- [7]. Shen C, et al. Structural insights into the allosteric inhibition of P2X4 receptors. Nat Commun. 2023 Oct 13;14(1):6437. [Content Brief]
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P2X4 Receptor Related Products (14)
Related Products (14)
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BzATP triethylammonium salt
0 ImagesCat. No.: HY-136254Purity: 99.19%BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively. BzATP triethylammonium salt is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively.
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5-BDBD
0 Images5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
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BX430
0 ImagesBX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
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NP-1815-PX sodium
0 ImagesNP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis).
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PSB-12054
0 ImagesPSB-12054 is a P2X4 receptor antagonist with IC50 values of 0.19 μM, 2.10 μM and 1.77 μM against human, rat and mouse receptors, respectively, and exhibits selectivity over other human P2X receptor subtypes. PSB-12054 inhibits ATP-induced calcium influx, suppresses shear stress-induced transverse Ca2+ wave generation, and elevates basal Ca2+ levels in rat atrial myocytes. PSB-12054 binds to the 5-HT2B receptor. PSB-12054 can be used in research related to neuropathic pain, traumatic brain injury, cerebral ischemia and spinal cord injury.
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MRS2339
0 ImagesCat. No.: HY-182642CAS No.: 436847-13-1MRS2339 is a ribose-modified nucleotide and a nucleotidase-resistant P2 receptor agonist. MRS2339 activates P2X4R. MRS2339 induces ionic currents via P2X receptors, reduces cardiomyocyte cross-sectional area and heart weight/body weight ratio, lacks vasodilatory activity, and extends the lifespan of mice with cardiomyopathy. MRS2339 can be used in research related to heart failure and cardiomyopathy.
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PSB-12062
0 ImagesSynonyms: N-(p-Methylphenylsulfonyl)phenoxazinePSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
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NF279
0 ImagesNF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC50 value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection.
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P2X4 antagonist-1
0 ImagesP2X4 antagonist-1 is a P2X4 receptor antagonist with an IC50 of 15 nM. P2X4 antagonist-1 inhibits ATP (HY-B2176)-induced calcium influx. P2X4 antagonist-1 can be used for the research of pain syndromes, endometriosis, cancer.
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P2X4 antagonist-4
0 ImagesCat. No.: HY-168474CAS No.: 3108486-39-8P2X4 antagonist-4 (compound 64) is a potent P2X4R antagonist with an IC50 value of 8 µM. P2X4 antagonist-4 blocks the ATP-induced NLRP3 inflammasome activation and release of IL-1β.
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P2X4 antagonist-2
0 ImagesCat. No.: HY-160677CAS No.: 2055601-24-4P2X4 antagonist-2 is an antagonist for P2X4 with an IC50 of 24 nM.
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