P2X2 Receptor
P2X2 receptor is an ATP-gated P2X ion channel subunit within the P2X1-P2X7 family, which assembles as homo- or heterotrimeric nonselective cation channels activated by extracellular ATP[1][2]. Mechanistically, P2X2R converts extracellular purinergic signaling into ion-channel gating, and its desensitization depends on opposing intracellular calcium and ATP effects; calcium facilitates desensitization, whereas intracellular ATP prevents this calcium action[3]. In neural development models, P2X2 expression and activity were linked to neurogenesis progression and neuronal phenotype determination in neural progenitor and P19 cell systems[4]. Compared with related isoforms, P2X2 differs from strongly desensitizing P2X3 because non-desensitizing P2X2 subunits can co-assemble with P2X3 in taste-bud afferent signaling[2]. Functional heteromerization of P2X2 and P2X3 has also been established in sensory neurons, providing a distinct electrophysiological context from P2X4/P2X7 coexpression[5]. For experimental applications, Cdk5 phosphorylates P2X2a at C-terminal threonine 372 and modulates channel gating, supporting kinase-based studies of P2X2-dependent pain signaling[6]. Pharmacological studies should distinguish P2X2 from P2X3/P2X2/3 targets because gastrointestinal and pain research includes P2X3/P2X2/3 antagonist AF-219 rather than a P2X2-selective tool[7].
References:
- [1]. Schmid R, et al. ATP-Gated P2X Receptor Channels: Molecular Insights into Functional Roles. Annu Rev Physiol. 2019 Feb 10;81:43-62. [Content Brief]
- [2]. Burnstock G, et al. ATP-gated P2X receptors in health and disease. Front Cell Neurosci. 2014 Jul 24;8:204. [Content Brief]
- [3]. Rokic MB, et al. Opposing Roles of Calcium and Intracellular ATP on Gating of the Purinergic P2X2 Receptor Channel. Int J Mol Sci. 2018 Apr 11;19(4):1161. [Content Brief]
- [4]. Ulrich H, et al. P2X receptors in maintenance and differentiation of neural progenitor cells. Neural Regen Res. 2014 Dec 1;9(23):2040-1. [Content Brief]
- [5]. Schneider M, et al. Interaction of Purinergic P2X4 and P2X7 Receptor Subunits. Front Pharmacol. 2017 Nov 22;8:860. [Content Brief]
- [6]. Coddou C, et al. Cyclin-dependent kinase 5 modulates the P2X2a receptor channel gating through phosphorylation of C-terminal threonine 372. Pain. 2017 Nov;158(11):2155-2168. [Content Brief]
- [7]. Ochoa-Cortes F, et al. Potential for developing purinergic drugs for gastrointestinal diseases. Inflamm Bowel Dis. 2014 Jul;20(7):1259-87. [Content Brief]
All Product Categories
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P2X2 Receptor Related Products (9)
Related Products (9)
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Minodronic acid
0 ImagesSynonyms: YM-529Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC50 of 3 nM, and also an antagonist of P2X2/3 receptors with an IC50 of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer.
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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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RO-3
0 ImagesCat. No.: HY-19978CAS No.: 1026582-88-6RO-3 is a potent, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7).
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Minodronic acid-d4
0 ImagesCat. No.: HY-16322SCAS No.: 1807367-80-1Synonyms: YM-529-d4Minodronic acid-d4 (YM-529-d4) is deuterium labeled Minodronic acid (HY-16322). Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC50 of 3 nM, and also an antagonist of P2X2/3 receptors with an IC50 of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer.
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TNP-GTP tetrasodium
0 ImagesCat. No.: HY-137609ASynonyms: TNP-Guanosine 5'-triphosphate tetrasodiumTNP-GTP tetrasodium is a fluorescently labeled GTP (HY-113225) derivative. TNP-GTP tetrasodium can inhibit glutamate dehydrogenase (Ki = 2.7 μM). TNP-GTP tetrasodium is an antagonist of the purinergic P2X2 and P2X2/3 receptors with IC50 values of 0.4 and 1.2 nM, respectively. TNP-GTP tetrasodium also inhibit rat soluble guanylyl cyclase (Ki = 11 nM).
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PPADS
0 ImagesCat. No.: HY-108960CAS No.: 149017-66-3PPADS is a P2X receptor (P2X Receptor) antagonist and a reversible competitive antagonist of NAADP receptors, with IC50 values of 68 nM (P2X1) and 214 nM (P2X3), respectively. PPADS alleviates pain-related behaviors in the central and peripheral nervous systems of mice after peripheral neuropathy, inhibits the overproduction of IL-1β, IL-6, iNOS and nNOS, and suppresses the hydrolytic activity of extracellular ATPase. PPADS blocks ATP-mediated inward currents on recombinant rat P2X1 and P2X3 receptors, and inhibits purinergic nerve stimulation-induced contraction of rabbit bladder detrusor muscle. PPADS is applicable to research related to neuropathic pain.
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HW091077
0 ImagesCat. No.: HY-178450CAS No.: 2766757-56-4HW091077 is a highly selective P2X3 receptor antagonist with an IC50 of 17 nM. HW091077 blocks ATP-induced calcium influx and cell depolarization to inhibit cough reflex pathways. HW091077 is promising for research of chronic cough.
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P2X2R antagonist-1
0 ImagesCat. No.: HY-184044CAS No.: 13112-05-5P2X2R antagonist-1 (compound 66) is a P2X2 receptor antagonist derived from Reactive Blue 4 (HY-125815). P2X2R antagonist-1 shows high selectivity for P2X4, P2X7, P2Y2, P2Y4, P2Y6 and P2Y12 receptors, moderate selectivity for P2X1 and P2X3 receptors, and exhibits higher potency toward homomeric P2X2 receptors than heteromeric P2X2/3 receptors. P2X2R antagonist-1 competitively inhibits ATP-mediated currents. P2X2R antagonist-1 can be used in research related to pain and urinary incontinence.
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P2X3 antagonist 40
0 ImagesCat. No.: HY-183056P2X3 antagonist 40 is a P2X3 antagonist with a human P2X3 receptor pIC50 < 4.52. P2X3 antagonist 40 can be used for research on ATP-mediated proinflammatory fingerprint, including overactive bladder, pain, and chronic cough.
