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Gene Review

P2rx1  -  purinergic receptor P2X, ligand-gated ion...

Rattus norvegicus

Synonyms: ATP receptor, P2X purinoceptor 1, P2X1, Purinergic receptor, RP-2 protein
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Disease relevance of P2rx1


Psychiatry related information on P2rx1

  • P2X3 receptor blockade raised the pressure and volume thresholds for the reflex, whereas P2X1 receptor blockade diminished motor activity associated with voiding [6].

High impact information on P2rx1

  • A P2X purinoceptor expressed by a subset of sensory neurons [7].
  • There is sequence similarity between the ATP receptor and RP-2, a gene activated in thymocytes undergoing programmed cell death [8].
  • These data provide compelling new evidence indicating that tubuloglomerular feedback signals are coupled to autoregulatory preglomerular vasoconstriction through ATP-mediated activation of P2X1 receptors [9].
  • Afferent arterioles from rats and P2X1 KO mice were examined using the juxtamedullary nephron technique [9].
  • Sensitivity to two of these antagonists (pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid and pyridoxal 5-phosphate) is restored by replacement of Glu249 by lysine, which occurs at the equivalent position in P2X1 and P2X2 receptors [10].

Chemical compound and disease context of P2rx1


Biological context of P2rx1

  • RP-2 and RP-8 are no longer detectable after 6 h postinduction, when apoptosis and mRNA degradation are evident in the culture [14].
  • Sequence analysis of RP-8 cDNA indicates the presence of a zinc finger domain suggestive of a possible DNA regulatory role for the RP-8 protein. cDNA sequence results on RP-2 classify the corresponding protein as an integral membrane protein [14].
  • The potency of compound 3 at the recombinant P2X1 receptor (IC50 10.2 +/- 2.6 microM) was lower than PPADS (IC50 98.5 +/- 5.5 nM) or iso-PPADS (IC50 42.5 +/- 17.5 nM), although unlike PPADS its effect was reversible with washout and surmountable [15].
  • In the excretory ducts of the testis (ductus epididymidis, vas deferens and its associated seminal vesicles), the major signals were seen with antibodies to P2X1 and P2X2 in the membranes of the smooth muscle layer, suggesting that these receptors are involved in the process of sperm transport and ejaculation [16].
  • These results indicate that the 27-amino-acid sequence (175-201) is important for protein trafficking to the membrane and for the formation of a functional P2X1 receptor [17].

Anatomical context of P2rx1

  • Similar (heteromeric) P2X subunits also formed trimers, as shown for co-expressed P2X1 and P2X2 subunits, which assembled efficiently to a P2X1+2 receptor that was exported to the plasma membrane [18].
  • In the present study, antibodies recognizing the subunits P2X1-P2X7 were applied together with the astroglial marker S100beta and nuclear labeling with Hoechst 33342 to investigate semiquantitatively the distribution of the whole set of P2X receptors in astrocytes of the juvenile rat hippocampus [19].
  • RESULTS: In both the bladder detrusor muscle and the ureteral muscle (as well as the accompanying arteries) P2X1 immunoreactivity was associated with the smooth muscle membranes [20].
  • Taken together, these results indicate that noradrenergic terminals of the rat hippocampus are equipped with presynaptic facilitatory P2X receptors, displaying a pharmacological profile similar to homomeric P2X1 and P2X3 receptors [21].
  • MATERIALS AND METHODS: Distribution of P2X receptor subtypes in rat bladder and ureter has been investigated using specific polyclonal antibodies to P2X1 through to P2X7 receptor subtypes with immunohistochemical methods [20].

Associations of P2rx1 with chemical compounds

  • However, none of the currently used P2X purinoceptor antagonists suramin, reactive blue 2 and PPADS blocked ATP evoked currents; in contrast their application resulted in potentiation of the agonist response [22].
  • All VRL1-immunoreactive cells and processes colocalized with somatostatin and purinergic P2X1 receptor-IR but not with tyrosine hydroxylase-IR [23].
  • However contractions evoked by potassium chloride (60 mm) were unaffected by methyl-beta-cyclodextrin and the inactive analogue alpha-cyclodextrin had no effect on P2X1 receptor-mediated currents or contractions [24].
  • To determine whether lipid raft association was essential for P2X1 receptor channel function we used the cholesterol-depleting agent methyl-beta-cyclodextrin (10 mm for 1 h) [24].
  • This led to a redistribution of the P2X1 receptor throughout the sucrose gradient and reduced P2X1 receptor-mediated (alpha,beta-methylene ATP, 10 microm) currents in HEK293 cells by >90% and contractions of the rat tail artery by approximately 50% [24].

Other interactions of P2rx1


Analytical, diagnostic and therapeutic context of P2rx1


  1. Differential distribution of two ATP-gated channels (P2X receptors) determined by immunocytochemistry. Vulchanova, L., Arvidsson, U., Riedl, M., Wang, J., Buell, G., Surprenant, A., North, R.A., Elde, R. Proc. Natl. Acad. Sci. U.S.A. (1996) [Pubmed]
  2. 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]
  3. P2X1 receptor subunit immunoreactivity and ATP-evoked fast currents in adult rat dorsal root ganglion neurons. Petruska, J.C., Mena, N., Nakatsuka, T., Cooper, B.Y., Johnson, R.D., Gu, J.G. Neuroreport (2000) [Pubmed]
  4. Increase in cardiac P2X1-and P2Y2-receptor mRNA levels in congestive heart failure. Hou, M., Malmsjö, M., Möller, S., Pantev, E., Bergdahl, A., Zhao, X.H., Sun, X.Y., Hedner, T., Edvinsson, L., Erlinge, D. Life Sci. (1999) [Pubmed]
  5. Short-term hyperthyroidism modulates adenosine receptors and catalytic activity of adenylate cyclase in adipocytes. Rapiejko, P.J., Malbon, C.C. Biochem. J. (1987) [Pubmed]
  6. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. King, B.F., Knowles, I.D., Burnstock, G., Ramage, A.G. Br. J. Pharmacol. (2004) [Pubmed]
  7. A P2X purinoceptor expressed by a subset of sensory neurons. Chen, C.C., Akopian, A.N., Sivilotti, L., Colquhoun, D., Burnstock, G., Wood, J.N. Nature (1995) [Pubmed]
  8. New structural motif for ligand-gated ion channels defined by an ionotropic ATP receptor. Brake, A.J., Wagenbach, M.J., Julius, D. Nature (1994) [Pubmed]
  9. Physiological role for P2X1 receptors in renal microvascular autoregulatory behavior. Inscho, E.W., Cook, A.K., Imig, J.D., Vial, C., Evans, R.J. J. Clin. Invest. (2003) [Pubmed]
  10. An antagonist-insensitive P2X receptor expressed in epithelia and brain. Buell, G., Lewis, C., Collo, G., North, R.A., Surprenant, A. EMBO J. (1996) [Pubmed]
  11. ATP receptor-mediated increase of Ca ionophore-stimulated arachidonic acid release from PC12 pheochromocytoma cells. Murayama, T., Oda, H., Watanabe, A., Nomura, Y. Jpn. J. Pharmacol. (1995) [Pubmed]
  12. Differential control of renal vs. adrenal sympathetic nerve activity by NTS A2a and P2x purinoceptors. Scislo, T.J., O'Leary, D.S. Am. J. Physiol. (1998) [Pubmed]
  13. Impaired Ca2+ signaling attenuates P2X receptor-mediated vasoconstriction of afferent arterioles in angiotensin II hypertension. Zhao, X., Cook, A.K., Field, M., Edwards, B., Zhang, S., Zhang, Z., Pollock, J.S., Imig, J.D., Inscho, E.W. Hypertension (2005) [Pubmed]
  14. Identification of mRNAs associated with programmed cell death in immature thymocytes. Owens, G.P., Hahn, W.E., Cohen, J.J. Mol. Cell. Biol. (1991) [Pubmed]
  15. A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors. Jacobson, K.A., Kim, Y.C., Wildman, S.S., Mohanram, A., Harden, T.K., Boyer, J.L., King, B.F., Burnstock, G. J. Med. Chem. (1998) [Pubmed]
  16. P2X receptor immunoreactivity in the male genital organs of the rat. Lee, H.Y., Bardini, M., Burnstock, G. Cell Tissue Res. (2000) [Pubmed]
  17. Presence and possible role of the spliced isoform of the P2X1 receptor in rat vascular smooth muscle cells. Ohkubo, T., Yamazaki, J., Nakashima, Y., Kitamura, K. Pflugers Arch. (2000) [Pubmed]
  18. Trimeric architecture of homomeric P2X2 and heteromeric P2X1+2 receptor subtypes. Aschrafi, A., Sadtler, S., Niculescu, C., Rettinger, J., Schmalzing, G. J. Mol. Biol. (2004) [Pubmed]
  19. Distribution of P2X receptors on astrocytes in juvenile rat hippocampus. Kukley, M., Barden, J.A., Steinhäuser, C., Jabs, R. Glia (2001) [Pubmed]
  20. Distribution of P2X receptors in the urinary bladder and the ureter of the rat. Lee, H.Y., Bardini, M., Burnstock, G. J. Urol. (2000) [Pubmed]
  21. P2X receptor activation elicits transporter-mediated noradrenaline release from rat hippocampal slices. Papp, L., Balázsa, T., Köfalvi, A., Erdélyi, F., Szabó, G., Vizi, E.S., Sperlágh, B. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  22. A P2X purinoceptor cDNA conferring a novel pharmacological profile. Bo, X., Zhang, Y., Nassar, M., Burnstock, G., Schoepfer, R. FEBS Lett. (1995) [Pubmed]
  23. Vanilloid receptor like 1 (VRL1) immunoreactivity in mammalian retina: colocalization with somatostatin and purinergic P2X1 receptors. Yazulla, S., Studholme, K.M. J. Comp. Neurol. (2004) [Pubmed]
  24. Disruption of lipid rafts inhibits P2X1 receptor-mediated currents and arterial vasoconstriction. Vial, C., Evans, R.J. J. Biol. Chem. (2005) [Pubmed]
  25. Purinergic signalling to rat ovarian smooth muscle: changes in P2X receptor expression during pregnancy. Katugampola, H., Burnstock, G. Cells Tissues Organs (Print) (2004) [Pubmed]
  26. The pattern of distribution of selected ATP-sensitive P2 receptor subtypes in normal rat kidney: an immunohistological study. Turner, C.M., Vonend, O., Chan, C., Burnstock, G., Unwin, R.J. Cells Tissues Organs (Print) (2003) [Pubmed]
  27. P2X4, P2Y1 and P2Y2 receptors on rat alveolar macrophages. Bowler, J.W., Bailey, R.J., North, R.A., Surprenant, A. Br. J. Pharmacol. (2003) [Pubmed]
  28. Gene expression of P2X-receptors in the developing inner ear of the rat. Brändle, U., Zenner, H.P., Ruppersberg, J.P. Neurosci. Lett. (1999) [Pubmed]
  29. Molecular cloning and functional expression of a novel rat heart P2X purinoceptor. Garcia-Guzman, M., Soto, F., Laube, B., Stühmer, W. FEBS Lett. (1996) [Pubmed]
  30. P2X (purinergic) receptor distributions in rat blood vessels. Hansen, M.A., Dutton, J.L., Balcar, V.J., Barden, J.A., Bennett, M.R. J. Auton. Nerv. Syst. (1999) [Pubmed]
  31. Localization of P2X purinoceptor transcripts in the rat nervous system. Kidd, E.J., Grahames, C.B., Simon, J., Michel, A.D., Barnard, E.A., Humphrey, P.P. Mol. Pharmacol. (1995) [Pubmed]
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