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Gene Review

P2RX2  -  purinergic receptor P2X, ligand gated ion...

Homo sapiens

Synonyms: ATP receptor, DFNA41, P2X purinoceptor 2, P2X2, Purinergic receptor
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Disease relevance of P2RX2


High impact information on P2RX2

  • Coexpression of P2X2 and P2X3 receptor subunits can account for ATP-gated currents in sensory neurons [6].
  • Brief (< 1 s) applications of ATP to nodose ganglion neurons or to cells transfected with P2X2 or P2X4 receptor cDNAs induce the opening of a channel selectively permeable to small cations within milliseconds [7].
  • This effect is enhanced in P2X2 receptors carrying point mutations in the second transmembrane segment [7].
  • In all of the cell lines tested, P2-purinergic receptor agonists, including ATP and certain hydrolysis-resistant adenine nucleotides, induced a rapid, transient increase in cytoplasmic free Ca2+ that was detectable at 50 to 100 nM ATP, was maximal at 100 microM ATP, and was inhibited approximately 50% by chelation of extracellular Ca2+ [8].
  • P2-purinergic receptor agonists inhibit the growth of androgen-independent prostate carcinoma cells [8].

Biological context of P2RX2

  • Inhibitors of the mitochondrial electron transport chain that reduce (rotenone and myxothiazol) or increase (antimycin A) the production of ROS altered the magnitude of P2X2-mediated currents [1].
  • A-317491 potently blocked recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and was highly selective (IC50 >10 microM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes [4].
  • When this region is removed, or when charge is added to it, P2X6 forms homotrimeric assemblies, undergoes complex glycosylation and is delivered to the plasma membrane, albeit less efficiently than the P2X2 receptor [9].
  • When alpha,beta-methylene ATP was the agonist (activating heteromeric P2X2/3 receptors), the inhibition by TNP-ATP conformed to a single binding site (half-maximal concentration about 3 nM) [10].
  • P2X2 expression was found in nuclei of rat facial motoneurons, with nuclear export in the cytoplasm after nerve resection [11].

Anatomical context of P2RX2

  • Human, rat, and mouse testicular smooth muscle demonstrated purinergic responsiveness, probably mediated through the P2X1 and/or P2X2 receptors [12].
  • In RT-PCR, circular myocytes expressed mRNAs encoding P2X2, 3 and 4, while longitudinal myocytes expressed mRNAs for P2X3 and 5 [13].
  • Labelling for each P2X subtype was seen in the apical, lateral and basal compartments on Days 1 and 3, except for P2X2 which was only observed in the basement membrane [14].
  • We also show a physical interaction between P2X2 and rho1 receptors expressed in oocytes and the co-clustering of these receptors in transfected hippocampal neurons [15].
  • Human erythrocytes expressed P2X7 receptors on all cells examined from eight of eight subjects, as well as P2X2 at a far lower staining intensity in six of eight subjects [16].

Associations of P2RX2 with chemical compounds


Other interactions of P2RX2

  • Each member of the family can form functional homomeric channels, but only P2X2 and P2X3 have been shown to combine to form a unique heteromeric channel [21].
  • In contrast, in the solitary tract and its nucleus (NTS), colocalization of P2X2- and P2X3-ir was seen at low and high magnification [22].

Analytical, diagnostic and therapeutic context of P2RX2

  • Atomic force microscopy imaging demonstrates that P2X2 receptors are trimers but that P2X6 receptor subunits do not oligomerize [23].
  • In cells expressing homomeric P2X2 receptors, perfusion of 5 microM ATP (EC25) induced an inward whole-cell current that showed little desensitization during repeated exposures under continuously normoxic conditions [1].
  • Whole-cell recordings from these cells showed that ATP and alphabetamethylene-ATP evoked currents with agonist sensitivity and desensitization quite distinct from those observed when P2X2 or P2X3 receptors were expressed alone [2].
  • Involvement of P2X1 and P2X2 purinergic receptors in motoneuron response to injury was investigated with Western blotting and immunohistochemistry and correlated with motoneuron loss, Bcl-2 expression, nitric oxide synthase induction and glial activation [11].
  • Furthermore, this paper demonstrates the role of quantitative structure-activity relationships (QSARs) in P2X research (calcium ion permeability of the wild-type and after site-directed mutagenesis of the rat P2X2 receptor protein, KN-62 analogs as competitive antagonists of the human P2X7 receptor) [24].


  1. Selective modulation of ligand-gated P2X purinoceptor channels by acute hypoxia is mediated by reactive oxygen species. Mason, H.S., Bourke, S., Kemp, P.J. Mol. Pharmacol. (2004) [Pubmed]
  2. Baculovirus expression provides direct evidence for heteromeric assembly of P2X2 and P2X3 receptors. Radford, K.M., Virginio, C., Surprenant, A., North, R.A., Kawashima, E. J. Neurosci. (1997) [Pubmed]
  3. A novel and efficient method for the stable expression of heteromeric ion channels in mammalian cells. Kawashima, E., Estoppey, D., Virginio, C., Fahmi, D., Rees, S., Surprenant, A., North, R.A. Recept. Channels (1998) [Pubmed]
  4. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Jarvis, M.F., Burgard, E.C., McGaraughty, S., Honore, P., Lynch, K., Brennan, T.J., Subieta, A., Van Biesen, T., Cartmell, J., Bianchi, B., Niforatos, W., Kage, K., Yu, H., Mikusa, J., Wismer, C.T., Zhu, C.Z., Chu, K., Lee, C.H., Stewart, A.O., Polakowski, J., Cox, B.F., Kowaluk, E., Williams, M., Sullivan, J., Faltynek, C. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  5. Retinoic acids increase P2X2 receptor expression through the 5'-flanking region of P2rx2 gene in rat phaeochromocytoma PC-12 cells. Tozaki-Saitoh, H., Koizumi, S., Sato, Y., Tsuda, M., Nagao, T., Inoue, K. Mol. Pharmacol. (2006) [Pubmed]
  6. Coexpression of P2X2 and P2X3 receptor subunits can account for ATP-gated currents in sensory neurons. Lewis, C., Neidhart, S., Holy, C., North, R.A., Buell, G., Surprenant, A. Nature (1995) [Pubmed]
  7. Pore dilation of neuronal P2X receptor channels. Virginio, C., MacKenzie, A., Rassendren, F.A., North, R.A., Surprenant, A. Nat. Neurosci. (1999) [Pubmed]
  8. P2-purinergic receptor agonists inhibit the growth of androgen-independent prostate carcinoma cells. Fang, W.G., Pirnia, F., Bang, Y.J., Myers, C.E., Trepel, J.B. J. Clin. Invest. (1992) [Pubmed]
  9. An uncharged region within the N terminus of the P2X6 receptor inhibits its assembly and exit from the endoplasmic reticulum. Ormond, S.J., Barrera, N.P., Qureshi, O.S., Henderson, R.M., Edwardson, J.M., Murrell-Lagnado, R.D. Mol. Pharmacol. (2006) [Pubmed]
  10. The antagonist trinitrophenyl-ATP reveals co-existence of distinct P2X receptor channels in rat nodose neurones. Thomas, S., Virginio, C., North, R.A., Surprenant, A. J. Physiol. (Lond.) (1998) [Pubmed]
  11. Changes in the expression of P2X1 and P2X2 purinergic receptors in facial motoneurons after nerve lesions in rodents and correlation with motoneuron degeneration. Kassa, R.M., Bentivoglio, M., Mariotti, R. Neurobiol. Dis. (2007) [Pubmed]
  12. Smooth muscle and purinergic contraction of the human, rabbit, rat, and mouse testicular capsule. Banks, F.C., Knight, G.E., Calvert, R.C., Turmaine, M., Thompson, C.S., Mikhailidis, D.P., Morgan, R.J., Burnstock, G. Biol. Reprod. (2006) [Pubmed]
  13. Differential expression of P2X-purinoceptor subtypes in circular and longitudinal muscle of canine colon. Lee, H.K., Ro, S., Keef, K.D., Kathy, K.D., Kim, Y.H., Kim, H.W., Horowitz, B., Sanders, K.M. Neurogastroenterol. Motil. (2005) [Pubmed]
  14. Distributional changes of purinergic receptor subtypes (P2X 1-7) in uterine epithelial cells during early pregnancy. Slater, N.M., Barden, J.A., Murphy, C.R. Histochem. J. (2000) [Pubmed]
  15. Cross-talk and co-trafficking between rho1/GABA receptors and ATP-gated channels. Boué-Grabot, E., Emerit, M.B., Toulmé, E., Séguéla, P., Garret, M. J. Biol. Chem. (2004) [Pubmed]
  16. Extracellular ATP increases cation fluxes in human erythrocytes by activation of the P2X7 receptor. Sluyter, R., Shemon, A.N., Barden, J.A., Wiley, J.S. J. Biol. Chem. (2004) [Pubmed]
  17. Ionic permeability of, and divalent cation effects on, two ATP-gated cation channels (P2X receptors) expressed in mammalian cells. Evans, R.J., Lewis, C., Virginio, C., Lundstrom, K., Buell, G., Surprenant, A., North, R.A. J. Physiol. (Lond.) (1996) [Pubmed]
  18. A comparison of the binding characteristics of recombinant P2X1 and P2X2 purinoceptors. Michel, A.D., Lundström, K., Buell, G.N., Surprenant, A., Valera, S., Humphrey, P.P. Br. J. Pharmacol. (1996) [Pubmed]
  19. Expression of functional purinergic receptors in pulmonary neuroepithelial bodies and their role in hypoxia chemotransmission. Fu, X.W., Nurse, C.A., Cutz, E. Biol. Chem. (2004) [Pubmed]
  20. Purinergic regulation of sound transduction and auditory neurotransmission. Housley, G.D., Jagger, D.J., Greenwood, D., Raybould, N.P., Salih, S.G., Järlebark, L.E., Vlajkovic, S.M., Kanjhan, R., Nikolic, P., Muñoz, D.J., Thorne, P.R. Audiol. Neurootol. (2002) [Pubmed]
  21. Co-expression of P2X1 and P2X5 receptor subunits reveals a novel ATP-gated ion channel. Torres, G.E., Haines, W.R., Egan, T.M., Voigt, M.M. Mol. Pharmacol. (1998) [Pubmed]
  22. Immunohistochemical study of the P2X2 and P2X3 receptor subunits in rat and monkey sensory neurons and their central terminals. Vulchanova, L., Riedl, M.S., Shuster, S.J., Buell, G., Surprenant, A., North, R.A., Elde, R. Neuropharmacology (1997) [Pubmed]
  23. Atomic force microscopy imaging demonstrates that P2X2 receptors are trimers but that P2X6 receptor subunits do not oligomerize. Barrera, N.P., Ormond, S.J., Henderson, R.M., Murrell-Lagnado, R.D., Edwardson, J.M. J. Biol. Chem. (2005) [Pubmed]
  24. Bridging the gap between structural bioinformatics and receptor research: the membrane-embedded, ligand-gated, P2X glycoprotein receptor. Mager, P.P., Weber, A., Illes, P. Current topics in medicinal chemistry. (2004) [Pubmed]
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