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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 2 | 399 | 17p13.2 | P2RX1 | purinergic receptor P2X 1 | 52 |
Mouse | 2 | 399 | 11 45.09 cM | P2rx1 | purinergic receptor P2X, ligand-gated ion channel, 1 | 29 |
Rat | 2 | 399 | 10q24 | P2rx1 | purinergic receptor P2X 1 | 51 |
Previous and Unofficial Names |
P2XR1 | P2X purinoceptor 1 | P2X1 receptor | Pdcd3 | purinergic receptor P2X, ligand gated ion channel, 1 | purinergic receptor P2X |
Database Links | |
Alphafold | P51575 (Hs), P51576 (Mm), P47824 (Rn) |
CATH/Gene3D | 2.60.490.10 |
ChEMBL Target | CHEMBL2094 (Hs), CHEMBL5496 (Mm), CHEMBL2530 (Rn) |
Ensembl Gene | ENSG00000108405 (Hs), ENSMUSG00000020787 (Mm), ENSRNOG00000017606 (Rn) |
Entrez Gene | 5023 (Hs), 18436 (Mm), 25505 (Rn) |
Human Protein Atlas | ENSG00000108405 (Hs) |
KEGG Gene | hsa:5023 (Hs), mmu:18436 (Mm), rno:25505 (Rn) |
OMIM | 600845 (Hs) |
Pharos | P51575 (Hs) |
RefSeq Nucleotide | NM_002558 (Hs), NM_008771 (Mm), NM_012997 (Rn), NM_001285415 (Rn) |
RefSeq Protein | NP_002549 (Hs), NP_032797 (Mm), NP_037129 (Rn), NP_001272344 (Rn) |
UniProtKB | P51575 (Hs), P51576 (Mm), P47824 (Rn) |
Wikipedia | P2RX1 (Hs) |
Natural/Endogenous Ligands |
ATP |
Download all structure-activity data for this target as a CSV file
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Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific antagonist tables |
Allosteric Modulators | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
Functional P2X1 receptors are expressed by healthy human eosinophils [64]. In these cells P2X1 receptor activation is involved in αMβ2 integrin-dependent adhesion. Responses of eosinophils from asthmatic patients are reduced, potentially by increased extracellular nucleotide concentration as detected in bronchoalveolar lavage fluids from patients with airway inflammations [10,15,30,42]. |
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Tissue Distribution Comments | ||||||||||
The commonly used anti-P2X1 receptor antibody may not be selective in neuronal tissues [1] and so studies using this approach have not been included. |
Physiological Functions | ||||||||
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Gene Expression and Pathophysiology | ||||||||||||
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Gene Expression and Pathophysiology Comments | ||||||||||||
Eosinophils from asthmatic patients exhibit impaired P2X1 receptor-mediated adhesion [64]. |
Biologically Significant Variants | ||||||||||||||
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General Comments |
An alternatively spliced variant of the rat P2X1 subunit, provisionally termed p2X1a which lacks function as a homomer has been described [37]. An inactive, naturally occurring human mutant dominant negative P2X receptor has also been reported [39]. |
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2. Banks FC, Knight GE, Calvert RC, Thompson CS, Morgan RJ, Burnstock G. (2006) The purinergic component of human vas deferens contraction. Fertil Steril, 85 (4): 932-9. [PMID:16580377]
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6. Chan CM, Unwin RJ, Bardini M, Oglesby IB, Ford AP, Townsend-Nicholson A, Burnstock G. (1998) Localization of P2X1 purinoceptors by autoradiography and immunohistochemistry in rat kidneys. Am J Physiol, 274 (4 Pt 2): F799-804. [PMID:9575906]
7. Collo G, North RA, Kawashima E, Merlo-Pich E, Neidhart S, Surprenant A, Buell G. (1996) Cloning OF P2X5 and P2X6 receptors and the distribution and properties of an extended family of ATP-gated ion channels. J Neurosci, 16 (8): 2495-507. [PMID:8786426]
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9. Erhardt JA, Toomey JR, Douglas SA, Johns DG. (2006) P2X1 stimulation promotes thrombin receptor-mediated platelet aggregation. J Thromb Haemost, 4 (4): 882-90. [PMID:16634759]
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15. Idzko M, Hammad H, van Nimwegen M, Kool M, Willart MA, Muskens F, Hoogsteden HC, Luttmann W, Ferrari D, Di Virgilio F et al.. (2007) Extracellular ATP triggers and maintains asthmatic airway inflammation by activating dendritic cells. Nat Med, 13 (8): 913-9. [PMID:17632526]
16. Inscho EW, Cook AK, Imig JD, Vial C, Evans RJ. (2003) Physiological role for P2X1 receptors in renal microvascular autoregulatory behavior. J Clin Invest, 112 (12): 1895-905. [PMID:14679185]
17. Jacobson KA, Jarvis MF, Williams M. (2002) Purine and pyrimidine (P2) receptors as drug targets. J Med Chem, 45 (19): 4057-93. [PMID:12213051]
18. Jacobson KA, Kim YC, Wildman SS, Mohanram A, Harden TK, Boyer JL, King BF, Burnstock G. (1998) A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors. J Med Chem, 41 (13): 2201-6. [PMID:9632352]
19. Jiang L, Bardini M, Keogh A, dos Remedios CG, Burnstock G. (2005) P2X1 receptors are closely associated with connexin 43 in human ventricular myocardium. Int J Cardiol, 98 (2): 291-7. [PMID:15686781]
20. Kassack MU, Braun K, Ganso M, Ullmann H, Nickel P, Böing B, Müller G, Lambrecht G. (2004) Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist. Eur J Med Chem, 39 (4): 345-57. [PMID:15072843]
21. Khanam T, Burnstock G. (2007) Changes in expression of P2X1 receptors and connexin 43 in the rat myometrium during pregnancy. Fertil Steril, 88 (4 Suppl): 1174-9. [PMID:17561003]
22. Kim YC, Brown SG, Harden TK, Boyer JL, Dubyak G, King BF, Burnstock G, Jacobson KA. (2001) Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors. J Med Chem, 44 (3): 340-9. [PMID:11462975]
23. King BF, Liu M, Pintor J, Gualix J, Miras-Portugal MT, Burnstock G. (1999) Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors. Br J Pharmacol, 128 (5): 981-8. [PMID:10556935]
24. Klapperstück M, Büttner C, Nickel P, Schmalzing G, Lambrecht G, Markwardt F. (2000) Antagonism by the suramin analogue NF279 on human P2X(1) and P2X(7) receptors. Eur J Pharmacol, 387 (3): 245-52. [PMID:10650169]
25. Lalo U, Pankratov Y, Wichert SP, Rossner MJ, North RA, Kirchhoff F, Verkhratsky A. (2008) P2X1 and P2X5 subunits form the functional P2X receptor in mouse cortical astrocytes. J Neurosci, 28 (21): 5473-80. [PMID:18495881]
26. Lamont C, Vainorius E, Wier WG. (2003) Purinergic and adrenergic Ca2+ transients during neurogenic contractions of rat mesenteric small arteries. J Physiol (Lond.), 549 (Pt 3): 801-8. [PMID:12740429]
27. Lecut C, Frederix K, Johnson DM, Deroanne C, Thiry M, Faccinetto C, Marée R, Evans RJ, Volders PG, Bours V et al.. (2009) P2X1 ion channels promote neutrophil chemotaxis through Rho kinase activation. J Immunol, 183 (4): 2801-9. [PMID:19635923]
28. Lewis CJ, Evans RJ. (2001) P2X receptor immunoreactivity in different arteries from the femoral, pulmonary, cerebral, coronary and renal circulations. J Vasc Res, 38 (4): 332-40. [PMID:11455204]
29. Liang SX, Jenkins NA, Gilbert DJ, Copeland NG, Phillips WD. (2001) Structure and chromosome location of the mouse P2X(1) purinoceptor gene (P2rx1). Cytogenet Cell Genet, 92 (3-4): 333-6. [PMID:11435708]
30. Lommatzsch M, Cicko S, Müller T, Lucattelli M, Bratke K, Stoll P, Grimm M, Dürk T, Zissel G, Ferrari D et al.. (2010) Extracellular adenosine triphosphate and chronic obstructive pulmonary disease. Am J Respir Crit Care Med, 181 (9): 928-34. [PMID:20093639]
31. Longhurst PA, Schwegel T, Folander K, Swanson R. (1996) The human P2x1 receptor: molecular cloning, tissue distribution, and localization to chromosome 17. Biochim Biophys Acta, 1308 (3): 185-8. [PMID:8809107]
32. Maître B, Magnenat S, Heim V, Ravanat C, Evans RJ, de la Salle H, Gachet C, Hechler B. (2015) The P2X1 receptor is required for neutrophil extravasation during lipopolysaccharide-induced lethal endotoxemia in mice. J Immunol, 194 (2): 739-49. [PMID:25480563]
33. Mironneau J, Coussin F, Morel JL, Barbot C, Jeyakumar LH, Fleischer S, Mironneau C. (2001) Calcium signalling through nucleotide receptor P2X1 in rat portal vein myocytes. J Physiol (Lond.), 536 (Pt 2): 339-50. [PMID:11600670]
34. Mulryan K, Gitterman DP, Lewis CJ, Vial C, Leckie BJ, Cobb AL, Brown JE, Conley EC, Buell G, Pritchard CA et al.. (2000) Reduced vas deferens contraction and male infertility in mice lacking P2X1 receptors. Nature, 403 (6765): 86-9. [PMID:10638758]
35. Nori S, Fumagalli L, Bo X, Bogdanov Y, Burnstock G. (1998) Coexpression of mRNAs for P2X1, P2X2 and P2X4 receptors in rat vascular smooth muscle: an in situ hybridization and RT-PCR study. J Vasc Res, 35 (3): 179-85. [PMID:9647332]
36. O'Reilly BA, Kosaka AH, Chang TK, Ford AP, Popert R, McMahon SB. (2001) A quantitative analysis of purinoceptor expression in the bladders of patients with symptomatic outlet obstruction. BJU Int, 87 (7): 617-22. [PMID:11350400]
37. Ohkubo T, Yamazaki J, Nakashima Y, Kitamura K. (2000) Presence and possible role of the spliced isoform of the P2X1 receptor in rat vascular smooth muscle cells. Pflugers Arch, 441 (1): 57-64. [PMID:11205062]
38. Oury C, Kuijpers MJ, Toth-Zsamboki E, Bonnefoy A, Danloy S, Vreys I, Feijge MA, De Vos R, Vermylen J, Heemskerk JW et al.. (2003) Overexpression of the platelet P2X1 ion channel in transgenic mice generates a novel prothrombotic phenotype. Blood, 101 (10): 3969-76. [PMID:12521992]
39. Oury C, Toth-Zsamboki E, Van Geet C, Thys C, Wei L, Nilius B, Vermylen J, Hoylaerts MF. (2000) A natural dominant negative P2X1 receptor due to deletion of a single amino acid residue. J Biol Chem, 275 (30): 22611-4. [PMID:10816552]
40. Przybyła T, Sakowicz-Burkiewicz M, Pawełczyk T. (2018) Purinergic signaling in B cells. Acta Biochim Pol, 65 (1): 1-7. [PMID:29360885]
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42. Riteau N, Gasse P, Fauconnier L, Gombault A, Couegnat M, Fick L, Kanellopoulos J, Quesniaux VF, Marchand-Adam S, Crestani B et al.. (2010) Extracellular ATP is a danger signal activating P2X7 receptor in lung inflammation and fibrosis. Am J Respir Crit Care Med, 182 (6): 774-83. [PMID:20522787]
43. Rodrigues RJ, Almeida T, Richardson PJ, Oliveira CR, Cunha RA. (2005) Dual presynaptic control by ATP of glutamate release via facilitatory P2X1, P2X2/3, and P2X3 and inhibitory P2Y1, P2Y2, and/or P2Y4 receptors in the rat hippocampus. J Neurosci, 25 (27): 6286-95. [PMID:16000618]
44. Scase TJ, Heath MF, Allen JM, Sage SO, Evans RJ. (1998) Identification of a P2X1 purinoceptor expressed on human platelets. Biochem Biophys Res Commun, 242 (3): 525-8. [PMID:9464249]
45. Silva AM, Rodrigues RJ, Tomé AR, Cunha RA, Misler S, Rosário LM, Santos RM. (2008) Electrophysiological and immunocytochemical evidence for P2X purinergic receptors in pancreatic beta cells. Pancreas, 36 (3): 279-83. [PMID:18362842]
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47. Sluyter R, Barden JA, Wiley JS. (2001) Detection of P2X purinergic receptors on human B lymphocytes. Cell Tissue Res, 304 (2): 231-6. [PMID:11396717]
48. Soto F, Lambrecht G, Nickel P, Stühmer W, Busch AE. (1999) Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors. Neuropharmacology, 38 (1): 141-9. [PMID:10193905]
49. Sánchez-Nogueiro J, Marín-García P, León D, León-Otegui M, Salas E, Gómez-Villafuertes R, Gualix J, Miras-Portugal MT. (2009) Axodendritic fibres of mouse cerebellar granule neurons exhibit a diversity of functional P2X receptors. Neurochem Int, 55 (7): 671-82. [PMID:19560503]
50. Vaeth M, Feske S. (2018) Ion channelopathies of the immune system. Curr Opin Immunol, 52: 39-50. [PMID:29635109]
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53. Vial C, Evans RJ. (2000) P2X receptor expression in mouse urinary bladder and the requirement of P2X(1) receptors for functional P2X receptor responses in the mouse urinary bladder smooth muscle. Br J Pharmacol, 131 (7): 1489-95. [PMID:11090125]
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58. Virginio C, Robertson G, Surprenant A, North RA. (1998) Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors. Mol Pharmacol, 53 (6): 969-73. [PMID:9614197]
59. Vulchanova L, Arvidsson U, Riedl M, Wang J, Buell G, Surprenant A, North RA, Elde R. (1996) Differential distribution of two ATP-gated channels (P2X receptors) determined by immunocytochemistry. Proc Natl Acad Sci USA, 93 (15): 8063-7. [PMID:8755603]
60. Wang L, Andersson M, Karlsson L, Watson MA, Cousens DJ, Jern S, Erlinge D. (2003) Increased mitogenic and decreased contractile P2 receptors in smooth muscle cells by shear stress in human vessels with intact endothelium. Arterioscler Thromb Vasc Biol, 23 (8): 1370-6. [PMID:12791671]
61. Wang L, Karlsson L, Moses S, Hultgårdh-Nilsson A, Andersson M, Borna C, Gudbjartsson T, Jern S, Erlinge D. (2002) P2 receptor expression profiles in human vascular smooth muscle and endothelial cells. J Cardiovasc Pharmacol, 40 (6): 841-53. [PMID:12451317]
62. Wang X, Qin W, Xu X, Xiong Y, Zhang Y, Zhang H, Sun B. (2017) Endotoxin-induced autocrine ATP signaling inhibits neutrophil chemotaxis through enhancing myosin light chain phosphorylation. Proc Natl Acad Sci USA, 114 (17): 4483-4488. [PMID:28396412]
63. Wareham K, Vial C, Wykes RC, Bradding P, Seward EP. (2009) Functional evidence for the expression of P2X1, P2X4 and P2X7 receptors in human lung mast cells. Br J Pharmacol, 157 (7): 1215-24. [PMID:19552691]
64. Wright A, Mahaut-Smith M, Symon F, Sylvius N, Ran S, Bafadhel M, Muessel M, Bradding P, Wardlaw A, Vial C. (2016) Impaired P2X1 Receptor-Mediated Adhesion in Eosinophils from Asthmatic Patients. J Immunol, 196 (12): 4877-84. [PMID:27183585]