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Gene Review

P2ry1  -  purinergic receptor P2Y, G-protein coupled 1

Mus musculus

Synonyms: ATP receptor, P2Y purinoceptor 1, P2Y1, P2Y1 receptor, Purinergic receptor
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Disease relevance of P2ry1

  • This report implicates the P2Z/P2X7 receptor in the control of protein kinase cascades and transcriptional processes, and these observations are likely to be important for the development of selective purinergic receptor antagonists for the treatment of septic shock [1].
  • P2Y1-deficient mice and mice treated with the P2Y1 antagonist MRS2179 displayed significantly less arterial thrombosis than their respective controls [2].
  • Previous studies in experimental models revealed a role for the P2Y1 platelet ADP receptor in systemic vascular thromboembolism models [2].
  • These results demonstrate a role for the P2Y1 receptor in both arterial and venous thrombosis, further establishing this receptor as a potential target for antithrombotic drugs [2].
  • 5. C6 glioma cells express a P2Y-purinoceptor that inhibits adenylyl cyclase but does not activate phospholipase C. Expression of the human P2Y1-purinoceptor in C6 cells conferred 2MeSATP-stimulated inositol lipid hydrolysis to these cells [3].

High impact information on P2ry1

  • We show here that the purinoceptor P2Y1 is required for platelet shape change in response to ADP and is also a principal receptor mediating ADP-induced platelet aggregation [4].
  • Decreased platelet aggregation, increased bleeding time and resistance to thromboembolism in P2Y1-deficient mice [4].
  • In vivo, the lack of P2Y1 expression increased bleeding time and protected from collagen- and ADP-induced thromboembolism [4].
  • The excitatory effects of medium samples and of ATP are blocked by purinergic receptor antagonists and by pretreatment with apyrase; these same purinergic receptor antagonists block propagation of electrically evoked calcium waves [5].
  • Since ADP, AMP, and adenosine (in descending order) were less potent or ineffective in inducing the cation conductance, the involvement of a P2 purinergic receptor is proposed [6].

Chemical compound and disease context of P2ry1

  • Inhibition of localized thrombosis in P2Y1-deficient mice and rodents treated with MRS2179, a P2Y1 receptor antagonist [2].
  • The P2Y1 receptor is a Galpha q coupled G-protein receptor that is important for platelet shape change, aggregation, thromboxane A2 generation, procoagulant activity, adhesion to immobilized fibrinogen and thrombus formation under shear conditions [7].

Biological context of P2ry1


Anatomical context of P2ry1


Associations of P2ry1 with chemical compounds

  • P2Y4 receptors were not involved, since P2Y4-deficient mice displayed unaltered responses to ATP and UTP.The purinergic receptor antagonist suramin exerted surmountable antagonism for all agonists [12].
  • The ATP/ATPgammaS-evoked relaxation and calcium signals in the knockout mice were partially rescued by P2Y1, as they were sensitive to 2'-deoxy-N6-methyladenosine 3',5'-bisphosphate (MRS2179), a P2Y1-selective antagonist.In contrast to ATP, the UTP-evoked relaxation was not different between knockout and WT mice [15].
  • Although depolarization enhanced Ca2+ mobilization resulting from GTPgammaS dialysis and to a lesser extent during AlF4- or thimerosal, these effects all required the presence of P2Y1 receptors [13].
  • The P2Y1 receptor is responsible for ADP-induced shape change and weak and transient aggregation, while the P2Y12 receptor is responsible for the completion and amplification of the response to ADP and to all platelet agonists, including thromboxane A2 (TXA2), thrombin, and collagen [16].
  • In platelets, the classical P2T receptor has now been resolved into three P2 receptor subtypes: the P2Y1, P2X1 and P2TAC receptors (the last of these, which is coupled to the inhibition of adenylate cyclase, is yet to be cloned) [17].

Physical interactions of P2ry1


Other interactions of P2ry1

  • Pharmacological screening with purinergic ligands indicated the presence of P2Y1 and P2Y2/4 receptors linked to the activation of a K+ current and P2X receptors, including P2X7, linked to the activation of a nonselective cationic current [19].
  • We identified the expression of most of the purinergic receptor subtypes (A1, A2, P2X1, 3-7, P2Y1, 2, 4) mRNAs, analysed by the reverse transcriptase-polymerase chain reaction [20].
  • A differential role of the platelet ADP receptors P2Y1 and P2Y12 in Rac activation [21].
  • Combination of P2Y1 deficiency with P2Y12 inhibition led to a significant additive effect [2].
  • 6 These results indicate the presence of several P2Y receptors coupled to an increase in intracellular calcium in the SCG: ADP-sensitive P2Y1 receptors and UDP-sensitive P2Y6 receptors in SCG neurons and glial cells, a novel UTP-sensitive P2Y receptor in SCG neurons and UTP- and ATP-sensitive P2Y2 receptors in SCG glia [14].

Analytical, diagnostic and therapeutic context of P2ry1


  1. Purinergic receptor modulation of lipopolysaccharide signaling and inducible nitric-oxide synthase expression in RAW 264.7 macrophages. Hu, Y., Fisette, P.L., Denlinger, L.C., Guadarrama, A.G., Sommer, J.A., Proctor, R.A., Bertics, P.J. J. Biol. Chem. (1998) [Pubmed]
  2. Inhibition of localized thrombosis in P2Y1-deficient mice and rodents treated with MRS2179, a P2Y1 receptor antagonist. Lenain, N., Freund, M., Léon, C., Cazenave, J.P., Gachet, C. J. Thromb. Haemost. (2003) [Pubmed]
  3. Second messenger cascade specificity and pharmacological selectivity of the human P2Y1-purinoceptor. Schachter, J.B., Li, Q., Boyer, J.L., Nicholas, R.A., Harden, T.K. Br. J. Pharmacol. (1996) [Pubmed]
  4. Decreased platelet aggregation, increased bleeding time and resistance to thromboembolism in P2Y1-deficient mice. Fabre, J.E., Nguyen, M., Latour, A., Keifer, J.A., Audoly, L.P., Coffman, T.M., Koller, B.H. Nat. Med. (1999) [Pubmed]
  5. ATP released from astrocytes mediates glial calcium waves. Guthrie, P.B., Knappenberger, J., Segal, M., Bennett, M.V., Charles, A.C., Kater, S.B. J. Neurosci. (1999) [Pubmed]
  6. Extracellular ATP activates a cation conductance and a K+ conductance in cultured microglial cells from mouse brain. Walz, W., Ilschner, S., Ohlemeyer, C., Banati, R., Kettenmann, H. J. Neurosci. (1993) [Pubmed]
  7. The role of ADP receptors in platelet function. Murugappa, S., Kunapuli, S.P. Front. Biosci. (2006) [Pubmed]
  8. Reduced expression of P2Y1 receptors in connexin43-null mice alters calcium signaling and migration of neural progenitor cells. Scemes, E., Duval, N., Meda, P. J. Neurosci. (2003) [Pubmed]
  9. Cloning and tissue distribution of the human P2Y1 receptor. Janssens, R., Communi, D., Pirotton, S., Samson, M., Parmentier, M., Boeynaems, J.M. Biochem. Biophys. Res. Commun. (1996) [Pubmed]
  10. Inhibition of platelet functions and thrombosis through selective or nonselective inhibition of the platelet P2 receptors with increasing doses of NF449 [4,4',4'',4'''-(carbonylbis(imino-5,1,3-benzenetriylbis-(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid octasodium salt]. Hechler, B., Magnenat, S., Zighetti, M.L., Kassack, M.U., Ullmann, H., Cazenave, J.P., Evans, R., Cattaneo, M., Gachet, C. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  11. Increased susceptibility of purinergic receptor-deficient mice to lung infection with Pseudomonas aeruginosa. Geary, C., Akinbi, H., Korfhagen, T., Fabre, J.E., Boucher, R., Rice, W. Am. J. Physiol. Lung Cell Mol. Physiol. (2005) [Pubmed]
  12. Pharmacological characterization of nucleotide P2Y receptors on endothelial cells of the mouse aorta. Guns, P.J., Korda, A., Crauwels, H.M., Van Assche, T., Robaye, B., Boeynaems, J.M., Bult, H. Br. J. Pharmacol. (2005) [Pubmed]
  13. Direct voltage control of signaling via P2Y1 and other Galphaq-coupled receptors. Martinez-Pinna, J., Gurung, I.S., Vial, C., Leon, C., Gachet, C., Evans, R.J., Mahaut-Smith, M.P. J. Biol. Chem. (2005) [Pubmed]
  14. Evidence for P2Y1, P2Y2, P2Y6 and atypical UTP-sensitive receptors coupled to rises in intracellular calcium in mouse cultured superior cervical ganglion neurons and glia. Calvert, J.A., Atterbury-Thomas, A.E., Leon, C., Forsythe, I.D., Gachet, C., Evans, R.J. Br. J. Pharmacol. (2004) [Pubmed]
  15. Endothelium-dependent relaxation evoked by ATP and UTP in the aorta of P2Y2-deficient mice. Guns, P.J., Van Assche, T., Fransen, P., Robaye, B., Boeynaems, J.M., Bult, H. Br. J. Pharmacol. (2006) [Pubmed]
  16. The platelet P2 receptors as molecular targets for old and new antiplatelet drugs. Gachet, C. Pharmacol. Ther. (2005) [Pubmed]
  17. P2 receptor subtypes in the cardiovascular system. Kunapuli, S.P., Daniel, J.L. Biochem. J. (1998) [Pubmed]
  18. Effects of extracellular ATP and adenosine on different thymocyte subsets: possible role of ATP-gated channels and G protein-coupled purinergic receptor. Apasov, S.G., Koshiba, M., Chused, T.M., Sitkovsky, M.V. J. Immunol. (1997) [Pubmed]
  19. Purinergic receptors on microglial cells: functional expression in acute brain slices and modulation of microglial activation in vitro. Boucsein, C., Zacharias, R., Färber, K., Pavlovic, S., Hanisch, U.K., Kettenmann, H. Eur. J. Neurosci. (2003) [Pubmed]
  20. Purinergic receptor ligands stimulate pro-opiomelanocortin gene expression in AtT-20 pituitary corticotroph cells. Zhao, L.F., Iwasaki, Y., Oki, Y., Tsugita, M., Taguchi, T., Nishiyama, M., Takao, T., Kambayashi, M., Hashimoto, K. J. Neuroendocrinol. (2006) [Pubmed]
  21. A differential role of the platelet ADP receptors P2Y1 and P2Y12 in Rac activation. Soulet, C., Hechler, B., Gratacap, M.P., Plantavid, M., Offermanns, S., Gachet, C., Payrastre, B. J. Thromb. Haemost. (2005) [Pubmed]
  22. Possible involvement of P2Y2 metabotropic receptors in ATP-induced transient receptor potential vanilloid receptor 1-mediated thermal hypersensitivity. Moriyama, T., Iida, T., Kobayashi, K., Higashi, T., Fukuoka, T., Tsumura, H., Leon, C., Suzuki, N., Inoue, K., Gachet, C., Noguchi, K., Tominaga, M. J. Neurosci. (2003) [Pubmed]
  23. Structural characterization and fine chromosomal mapping of the human P2Y1 purinergic receptor gene (P2RY1). Ayyanathan, K., Naylor, S.L., Kunapuli, S.P. Somat. Cell Mol. Genet. (1996) [Pubmed]
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