P2X7

Target id: 484

Nomenclature: P2X7

Family: P2X receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for P2X7 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 595 12q24 P2RX7 purinergic receptor P2X 7 58
Mouse 2 595 5 P2rx7 purinergic receptor P2X, ligand-gated ion channel, 7 12
Rat 2 595 12q16 P2rx7 purinergic receptor P2X 7 72
Previous and Unofficial Names
P2X purinoceptor 7 | P2Z receptor | P2X7 receptor | purinergic receptor P2X, ligand gated ion channel, 7
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
ATP

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
ATP Hs Agonist 3.1 pEC50 37
pEC50 3.1 (EC50 7.8x10-4 M) [37]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
AZ11657312 (salt free) Rn Antagonist 7.8 pA2 3
pA2 7.8 [3]
decavanadate Hs Antagonist 7.4 pA2 50
pA2 7.4 pA2 = 7.4 [50]
AZ11657312 (salt free) Hs Antagonist 6.1 pA2 3
pA2 6.1 [3]
AZ10606120 Hs Antagonist 8.9 pKd 47
pKd 8.9 (Kd 1.4x10-9 M) [47]
Description: Measuring binding of [3H]-AZ10606120 to human P2X7 receptors
AZ10606120 Rn Antagonist 8.7 pKd 47
pKd 8.7 (Kd 1.9x10-9 M) [47]
Description: Measuring binding of [3H]-AZ10606120 to rat P2X7 receptors
JNJ-479655 Hs Antagonist 7.9 pKi 6
pKi 7.9 (Ki 1.26x10-8 M) [6]
A804598 Hs Antagonist ~8.0 pIC50
pIC50 ~8.0 (IC50 ~1x10-8 M)
brilliant blue G Hs Antagonist ~8.0 pIC50 38
pIC50 ~8.0 (IC50 ~1x10-8 M) [38]
A839977 Hs Antagonist ~7.7 pIC50 19-20,35
pIC50 ~7.7 (IC50 ~2x10-8 M) [19-20,35]
A740003 Hs Antagonist 7.4 pIC50 36
pIC50 7.4 (IC50 4x10-8 M) [36]
A438079 Hs Antagonist ~6.9 pIC50 19
pIC50 ~6.9 (IC50 ~1.25x10-7 M) [19]
PF-04905428 Hs Antagonist - - 18,21
[18,21]
View species-specific antagonist tables
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
chelerythrine Hs Negative 5.3 pIC50 - no 63
pIC50 5.3 (IC50 5.6x10-6 M) [63]
Not voltage dependent
Description: Inhibition of ATP-induced 86Rb+ (K+) efflux in human B-lymphocytes
ivermectin Hs Positive - - - no 54
[54]
Not voltage dependent
AZ11645373 Hs Negative - - - no 49,70
[49,70]
Not voltage dependent
KN62 Hs Negative - - - no 27,63
[27,63]
Not voltage dependent
AZ10606120 Hs Negative - - - no 47
[47]
Not voltage dependent
[47]
Not voltage dependent
GW791343 Hs Negative - - - no 47-48
[47-48]
Not voltage dependent
GW791343 Rn Positive - - - no 47-48
[47-48]
Not voltage dependent
View species-specific allosteric modulator tables
Allosteric Modulator Comments
Effects of the allosteric regulators at P2X7 receptors are species-dependent. See Michel et al. (2008) [48] for an explanation.
No affinity data has been published quantifying the complex interaction of GW791343 with the P2X7 receptor. We have included the interaction in the table above based on extensive experimental evidence provided in [47] and [48].
Tissue Distribution
Bladder, astrocytes
Expression level:  Low
Species:  Human
Technique:  RT-PCR
References:  52,55
Brain, lung, prostate, leukocytes
Expression level:  Medium
Species:  Human
Technique:  Northern blot
References:  58
Fibroblasts; dendritic cells, osteoblasts, B lymphocytes, T lymphocytes, keratinocytes, erithrocytes, microglia
Expression level:  Medium
Species:  Human
Technique:  RT-PCR, Western blot, flow cytometry, immunohistochemistry, immunofluorescence
References:  5,9,28,30,66-68,77-78
Heart, liver, skeletal muscle, pancreas, thymus, tonsils, monocytes, macrophages, osteoclasts
Expression level:  High
Species:  Human
Technique:  Immunohistochemistry, Northern blot; flow cytometry; RT-PCR
References:  9,28,58
Bone marrow, macrophages, granulocytes, B lymphocytes, mast cells, submandibular glands, lung, microglia, Schwann cells, kidney, osteoclasts, osteoblasts, liver
Expression level:  High
Species:  Mouse
Technique:  In situ hybridisation, RT-PCR, Western blot, Immunofluorescence
References:  10,12,14-15,22,24,31-32,40,64
Bone marrow, macrophages, osteoclasts
Expression level:  High
Species:  Rat
Technique:  in situ hybridization
References:  14,51
New born brain, lung, spleen, bone marrow, spleen, salivary glands, testis, brain (ependyma,neurons from olfactory nucleus, cerebral cortex, piriform cortex, lateral septal nucleus, hippocampal pyramidal cells, oligodendrocytes, microglia), retina, parotid gland, lacrimal glands, pancreas, liver.
Expression level:  High
Species:  Rat
Technique:  in situ hybridization, RT-PCR, Northern Blot, Western blot, Immunofluorescence, Immunohistochemistry
References:  8,14,16,22,25,34,71,74,79
Physiological Consequences of Altering Gene Expression
Decreased proliferation
Species:  Mouse
Tissue:  microglia
Technique:  RNAi
References:  7
Defective IL-1 release; defective intraphagosomal killing
Species:  Mouse
Tissue:  macrophages, microglia
Technique:  Knock-out
References:  23,61,69
Reduced experimental arthritis, defective bone homeostasis; reduced neuropathic pain; reduced autoimmune hepatitis, reduced inflammation and fibrosis following ureteral obstruction, reduced experimental glomerulonephritis, defective wound healing, defective experimental encephalitis; reduced smoke-induced lung inflammation
Species:  Mouse
Tissue:  joint tissue, long bones, nervous system; liver, kidney, cornea, brain, lung
Technique:  Knock-out
References:  11,29,39-40,42,45-46,62,73
Anti-depressant-like behaviour, spatial memory impairment
Species:  Mouse
Tissue:  brain
Technique:  Knock-out
References:  4,43
Reduced long term potentiation and allodynia
Species:  Rat
Tissue:  spinal cord
Technique:  RNAi
References:  13
Gene Expression and Pathophysiology
Upregulation
Tissue or cell type:  B lymphocytes
Pathophysiology:  Chronic lymphocytic leukemia
Species:  Human
Technique:  RT-PCR, Western blot
References:  1
Upregulation
Tissue or cell type:  Kidney
Pathophysiology:  Experimental diabetes/hypertension
Species:  Mouse
Technique:  Immunohistochemistry, Western blotting
References:  75
Upregulation
Tissue or cell type:  Kidney
Pathophysiology:  Autosomal recessive polycystic kidney disease
Species:  Human
Technique:  Immunocytochemistry
References:  33
Upregulation
Tissue or cell type:  Retina
Pathophysiology:  Retinal degeneration
Species:  Mouse
Technique:  RT-PCR, immunohistochemistry
References:  26
Upregulation
Tissue or cell type:  Neuroblastoma cells
Pathophysiology:  Carcinomas
Species:  Human
Technique:  Immunohistochemistry
References:  57
Upregulation
Tissue or cell type:  Spinal cord
Pathophysiology:  Multiple sclerosis, Amiotrophic lateral sclerosis
Species:  Human
Technique:  Immunocytochemistry, Western blotting
References:  77
Upregulation
Tissue or cell type:  Microglia
Pathophysiology:  Mouse model of Alzheimer's disease
Species:  Mouse
Technique:  Immunofluorescence
References:  56
Biologically Significant Variants
Type:  Single nucleotide polymorphism
Species:  Mouse
Description:  Allelic mutation in the COOH tail of C57BL/6 and DBA mice decreases sensitivity to ATP
References:  2
Type:  Splice variant
Species:  Mouse
Description:  Alternative transmembrane domain 1. This variant escapes gene inactivation in P2X7 knock-out mice
Amino acids:  592
Nucleotide accession: 
Protein accession: 
References:  53
Type:  Single nucleotide polymorphism
Species:  Human
Description:  Splice site mutation at position +1 in intron 1, SNP 151+1g>t (rs35933842:- null allele)
References:  65
General Comments
The role of P2X7 receptor in cancer is discussed in [17].

References

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1. Adinolfi E, Melchiorri L, Falzoni S, Chiozzi P, Morelli A, Tieghi A, Cuneo A, Castoldi G, Di Virgilio F, Baricordi OR. (2002) P2X7 receptor expression in evolutive and indolent forms of chronic B lymphocytic leukemia. Blood99 (2): 706-8. [PMID:11781259]

2. Adriouch S, Dox C, Welge V, Seman M, Koch-Nolte F, Haag F. (2002) Cutting edge: a natural P451L mutation in the cytoplasmic domain impairs the function of the mouse P2X7 receptor. J. Immunol.169 (8): 4108-12. [PMID:12370338]

3. AstraZeneca. AZ11657312. Accessed on 12/09/2014. Modified on 12/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/az11657312/

4. Basso AM, Bratcher NA, Harris RR, Jarvis MF, Decker MW, Rueter LE. (2009) Behavioral profile of P2X7 receptor knockout mice in animal models of depression and anxiety: relevance for neuropsychiatric disorders. Behav. Brain Res.198 (1): 83-90. [PMID:18996151]

5. Berchtold S, Ogilvie AL, Bogdan C, Mühl-Zürbes P, Ogilvie A, Schuler G, Steinkasserer A. (1999) Human monocyte derived dendritic cells express functional P2X and P2Y receptors as well as ecto-nucleotidases. FEBS Lett.458 (3): 424-8. [PMID:10570953]

6. Bhattacharya A, Wang Q, Ao H, Shoblock JR, Lord B, Aluisio L, Fraser I, Nepomuceno D, Neff RA, Welty N et al.. (2013) Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br. J. Pharmacol.170 (3): 624-40. [PMID:23889535]

7. Bianco F, Ceruti S, Colombo A, Fumagalli M, Ferrari D, Pizzirani C, Matteoli M, Di Virgilio F, Abbracchio MP, Verderio C. (2006) A role for P2X7 in microglial proliferation. J. Neurochem.99 (3): 745-58. [PMID:16836656]

8. Brändle U, Kohler K, Wheeler-Schilling TH. (1998) Expression of the P2X7-receptor subunit in neurons of the rat retina. Brain Res. Mol. Brain Res.62 (1): 106-9. [PMID:9795168]

9. Buell G, Chessell IP, Michel AD, Collo G, Salazzo M, Herren S, Gretener D, Grahames C, Kaur R, Kosco-Vilbois MH, Humphrey PP. (1998) Blockade of human P2X7 receptor function with a monoclonal antibody. Blood92 (10): 3521-8. [PMID:9808543]

10. Bulanova E, Budagian V, Orinska Z, Hein M, Petersen F, Thon L, Adam D, Bulfone-Paus S. (2005) Extracellular ATP induces cytokine expression and apoptosis through P2X7 receptor in murine mast cells. J. Immunol.174 (7): 3880-90. [PMID:15778342]

11. Chessell IP, Hatcher JP, Bountra C, Michel AD, Hughes JP, Green P, Egerton J, Murfin M, Richardson J, Peck WL, Grahames CB, Casula MA, Yiangou Y, Birch R, Anand P, Buell GN. (2005) Disruption of the P2X7 purinoceptor gene abolishes chronic inflammatory and neuropathic pain. Pain114 (3): 386-96. [PMID:15777864]

12. Chessell IP, Simon J, Hibell AD, Michel AD, Barnard EA, Humphrey PP. (1998) Cloning and functional characterisation of the mouse P2X7 receptor. FEBS Lett.439 (1-2): 26-30. [PMID:9849870]

13. Chu YX, Zhang Y, Zhang YQ, Zhao ZQ. (2010) Involvement of microglial P2X7 receptors and downstream signaling pathways in long-term potentiation of spinal nociceptive responses. Brain Behav. Immun.24 (7): 1176-89. [PMID:20554014]

14. Collo G, Neidhart S, Kawashima E, Kosco-Vilbois M, North RA, Buell G. (1997) Tissue distribution of the P2X7 receptor. Neuropharmacology36 (9): 1277-83. [PMID:9364482]

15. Colomar A, Amédée T. (2001) ATP stimulation of P2X(7) receptors activates three different ionic conductances on cultured mouse Schwann cells. Eur. J. Neurosci.14 (6): 927-36. [PMID:11595031]

16. Coutinho-Silva R, Parsons M, Robson T, Lincoln J, Burnstock G. (2003) P2X and P2Y purinoceptor expression in pancreas from streptozotocin-diabetic rats. Mol. Cell. Endocrinol.204 (1-2): 141-54. [PMID:12850289]

17. Di Virgilio F. (2016) P2RX7: A receptor with a split personality in inflammation and cancer. Mol Cell Oncol3 (2): e1010937. [PMID:27308580]

18. Dombroski MA, Duplantier AJ. (2005) Benzamide inhibitors of the P2X7 receptor. Patent number: US6974812 B2. Assignee: Pfizer Inc.. Priority date: 31/12/2002. Publication date: 13/12/2005.

19. Donnelly-Roberts DL, Jarvis MF. (2007) Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. Br. J. Pharmacol.151 (5): 571-9. [PMID:17471177]

20. Donnelly-Roberts DL, Namovic MT, Han P, Jarvis MF. (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br. J. Pharmacol.157 (7): 1203-14. [PMID:19558545]

21. Duplantier AJ, Dombroski MA, Subramanyam C, Beaulieu AM, Chang SP, Gabel CA, Jordan C, Kalgutkar AS, Kraus KG, Labasi JM et al.. (2011) Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. Bioorg. Med. Chem. Lett.21 (12): 3708-11. [PMID:21565499]

22. Emmett DS, Feranchak A, Kilic G, Puljak L, Miller B, Dolovcak S, McWilliams R, Doctor RB, Fitz JG. (2008) Characterization of ionotrophic purinergic receptors in hepatocytes. Hepatology47 (2): 698-705. [PMID:18027885]

23. Fairbairn IP, Stober CB, Kumararatne DS, Lammas DA. (2001) ATP-mediated killing of intracellular mycobacteria by macrophages is a P2X(7)-dependent process inducing bacterial death by phagosome-lysosome fusion. J. Immunol.167 (6): 3300-7. [PMID:11544318]

24. Ferrari D, Chiozzi P, Falzoni S, Dal Susino M, Collo G, Buell G, Di Virgilio F. (1997) ATP-mediated cytotoxicity in microglial cells. Neuropharmacology36 (9): 1295-301. [PMID:9364484]

25. Franke H, Günther A, Grosche J, Schmidt R, Rossner S, Reinhardt R, Faber-Zuschratter H, Schneider D, Illes P. (2004) P2X7 receptor expression after ischemia in the cerebral cortex of rats. J. Neuropathol. Exp. Neurol.63 (7): 686-99. [PMID:15290894]

26. Franke H, Klimke K, Brinckmann U, Grosche J, Francke M, Sperlagh B, Reichenbach A, Liebert UG, Illes P. (2005) P2X(7) receptor-mRNA and -protein in the mouse retina; changes during retinal degeneration in BALBCrds mice. Neurochem. Int.47 (4): 235-42. [PMID:15964665]

27. Gargett CE, Wiley JS. (1997) The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes. Br. J. Pharmacol.120 (8): 1483-90. [PMID:9113369]

28. Gartland A, Buckley KA, Bowler WB, Gallagher JA. (2003) Blockade of the pore-forming P2X7 receptor inhibits formation of multinucleated human osteoclasts in vitro. Calcif. Tissue Int.73 (4): 361-9. [PMID:12874700]

29. Gonçalves RG, Gabrich L, Rosário A, Takiya CM, Ferreira ML, Chiarini LB, Persechini PM, Coutinho-Silva R, Leite M. (2006) The role of purinergic P2X7 receptors in the inflammation and fibrosis of unilateral ureteral obstruction in mice. Kidney Int.70 (9): 1599-606. [PMID:16969386]

30. Greig AV, Linge C, Terenghi G, McGrouther DA, Burnstock G. (2003) Purinergic receptors are part of a functional signaling system for proliferation and differentiation of human epidermal keratinocytes. J. Invest. Dermatol.120 (6): 1007-15. [PMID:12787128]

31. Grol MW, Panupinthu N, Korcok J, Sims SM, Dixon SJ. (2009) Expression, signaling, and function of P2X7 receptors in bone. Purinergic Signal.5 (2): 205-21. [PMID:19224395]

32. Hillman KA, Johnson TM, Winyard PJ, Burnstock G, Unwin RJ, Woolf AS. (2002) P2X(7) receptors are expressed during mouse nephrogenesis and in collecting duct cysts of the cpk/cpk mouse. Exp. Nephrol.10 (1): 34-42. [PMID:11803203]

33. Hillman KA, Woolf AS, Johnson TM, Wade A, Unwin RJ, Winyard PJ. (2004) The P2X7 ATP receptor modulates renal cyst development in vitro. Biochem. Biophys. Res. Commun.322 (2): 434-9. [PMID:15325248]

34. Hodges RR, Vrouvlianis J, Shatos MA, Dartt DA. (2009) Characterization of P2X7 purinergic receptors and their function in rat lacrimal gland. Invest. Ophthalmol. Vis. Sci.50 (12): 5681-9. [PMID:19608535]

35. Honore P, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y et al.. (2009) The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav. Brain Res.204 (1): 77-81. [PMID:19464323]

36. Honore P, Donnelly-Roberts D, Namovic MT, Hsieh G, Zhu CZ, Mikusa JP, Hernandez G, Zhong C, Gauvin DM, Chandran P et al.. (2006) A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J. Pharmacol. Exp. Ther.319 (3): 1376-85. [PMID:16982702]

37. Jacobson KA, Jarvis MF, Williams M. (2002) Purine and pyrimidine (P2) receptors as drug targets. J. Med. Chem.45 (19): 4057-93. [PMID:12213051]

38. Jiang LH, Mackenzie AB, North RA, Surprenant A. (2000) Brilliant blue G selectively blocks ATP-gated rat P2X(7) receptors. Mol. Pharmacol.58 (1): 82-8. [PMID:10860929]

39. Kawamura H, Aswad F, Minagawa M, Govindarajan S, Dennert G. (2006) P2X7 receptors regulate NKT cells in autoimmune hepatitis. J. Immunol.176 (4): 2152-60. [PMID:16455971]

40. Ke HZ, Qi H, Weidema AF, Zhang Q, Panupinthu N, Crawford DT, Grasser WA, Paralkar VM, Li M, Audoly LP, Gabel CA, Jee WS, Dixon SJ, Sims SM, Thompson DD. (2003) Deletion of the P2X7 nucleotide receptor reveals its regulatory roles in bone formation and resorption. Mol. Endocrinol.17 (7): 1356-67. [PMID:12677010]

41. Khalafalla MG, Woods LT, Camden JM, Khan AA, Limesand KH, Petris MJ, Erb L, Weisman GA. (2017) P2X7 receptor antagonism prevents IL-1β release from salivary epithelial cells and reduces inflammation in a mouse model of autoimmune exocrinopathy. J. Biol. Chem.,  [Epub ahead of print]. [PMID:28798231]

42. Labasi JM, Petrushova N, Donovan C, McCurdy S, Lira P, Payette MM, Brissette W, Wicks JR, Audoly L, Gabel CA. (2002) Absence of the P2X7 receptor alters leukocyte function and attenuates an inflammatory response. J. Immunol.168 (12): 6436-45. [PMID:12055263]

43. Labrousse VF, Costes L, Aubert A, Darnaudéry M, Ferreira G, Amédée T, Layé S. (2009) Impaired interleukin-1beta and c-Fos expression in the hippocampus is associated with a spatial memory deficit in P2X(7) receptor-deficient mice. PLoS ONE4 (6): e6006. [PMID:19547756]

44. Lister MF, Sharkey J, Sawatzky DA, Hodgkiss JP, Davidson DJ, Rossi AG, Finlayson K. (2007) The role of the purinergic P2X7 receptor in inflammation. J Inflamm (Lond)4: 5. [PMID:17367517]

45. Lucattelli M, S, T, M, G, S, W, M, R, T, G, S, D, F, JC, G, M. (2010) P2X7 Receptor Signalling in the Pathogenesis of Smoke-induced Lung Inflammation and Emphysema. Am J Respir Cell Mol Biol, . [PMID:20508069]

46. Mayo C, Ren R, Rich C, Stepp MA, Trinkaus-Randall V. (2008) Regulation by P2X7: epithelial migration and stromal organization in the cornea. Invest. Ophthalmol. Vis. Sci.49 (10): 4384-91. [PMID:18502993]

47. Michel AD, Chambers LJ, Walter DS. (2008) Negative and positive allosteric modulators of the P2X(7) receptor. Br. J. Pharmacol.153 (4): 737-50. [PMID:18071294]

48. Michel AD, Clay WC, Ng SW, Roman S, Thompson K, Condreay JP, Hall M, Holbrook J, Livermore D, Senger S. (2008) Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects. Br. J. Pharmacol.155 (5): 738-51. [PMID:18660826]

49. Michel AD, Ng SW, Roman S, Clay WC, Dean DK, Walter DS. (2009) Mechanism of action of species-selective P2X(7) receptor antagonists. Br. J. Pharmacol.156 (8): 1312-25. [PMID:19309360]

50. Michel AD, Xing M, Thompson KM, Jones CA, Humphrey PP. (2006) Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors. Eur. J. Pharmacol.534 (1-3): 19-29. [PMID:16487507]

51. Naemsch LN, Dixon SJ, Sims SM. (2001) Activity-dependent development of P2X7 current and Ca2+ entry in rabbit osteoclasts. J. Biol. Chem.276 (42): 39107-14. [PMID:11495918]

52. Narcisse L, Scemes E, Zhao Y, Lee SC, Brosnan CF. (2005) The cytokine IL-1beta transiently enhances P2X7 receptor expression and function in human astrocytes. Glia49 (2): 245-58. [PMID:15472991]

53. Nicke A, Kuan YH, Masin M, Rettinger J, Marquez-Klaka B, Bender O, Górecki DC, Murrell-Lagnado RD, Soto F. (2009) A functional P2X7 splice variant with an alternative transmembrane domain 1 escapes gene inactivation in P2X7 knock-out mice. J. Biol. Chem.284 (38): 25813-22. [PMID:19546214]

54. Nörenberg W, Sobottka H, Hempel C, Plötz T, Fischer W, Schmalzing G, Schaefer M. (2012) Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors. Br. J. Pharmacol.167 (1): 48-66. [PMID:22506590]

55. O'Reilly BA, Kosaka AH, Chang TK, Ford AP, Popert R, Rymer JM, McMahon SB. (2001) A quantitative analysis of purinoceptor expression in human fetal and adult bladders. J. Urol.165 (5): 1730-4. [PMID:11342965]

56. Parvathenani LK, Tertyshnikova S, Greco CR, Roberts SB, Robertson B, Posmantur R. (2003) P2X7 mediates superoxide production in primary microglia and is up-regulated in a transgenic mouse model of Alzheimer's disease. J. Biol. Chem.278 (15): 13309-17. [PMID:12551918]

57. Raffaghello L, Chiozzi P, Falzoni S, Di Virgilio F, Pistoia V. (2006) The P2X7 receptor sustains the growth of human neuroblastoma cells through a substance P-dependent mechanism. Cancer Res.66 (2): 907-14. [PMID:16424024]

58. Rassendren F, Buell GN, Virginio C, Collo G, North RA, Surprenant A. (1997) The permeabilizing ATP receptor, P2X7. Cloning and expression of a human cDNA. J. Biol. Chem.272 (9): 5482-6. [PMID:9038151]

59. Rathinam VA, Fitzgerald KA. (2016) Inflammasome Complexes: Emerging Mechanisms and Effector Functions. Cell165 (4): 792-800. [PMID:27153493]

60. 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]

61. Sanz JM, Chiozzi P, Ferrari D, Colaianna M, Idzko M, Falzoni S, Fellin R, Trabace L, Di Virgilio F. (2009) Activation of microglia by amyloid {beta} requires P2X7 receptor expression. J. Immunol.182 (7): 4378-85. [PMID:19299738]

62. Sharp AJ, Polak PE, Simonini V, Lin SX, Richardson JC, Bongarzone ER, Feinstein DL. (2008) P2x7 deficiency suppresses development of experimental autoimmune encephalomyelitis. J Neuroinflammation5: 33. [PMID:18691411]

63. Shemon AN, Sluyter R, Conigrave AD, Wiley JS. (2004) Chelerythrine and other benzophenanthridine alkaloids block the human P2X7 receptor. Br. J. Pharmacol.142 (6): 1015-9. [PMID:15210579]

64. Sim JA, Young MT, Sung HY, North RA, Surprenant A. (2004) Reanalysis of P2X7 receptor expression in rodent brain. J. Neurosci.24 (28): 6307-14. [PMID:15254086]

65. Skarratt KK, Fuller SJ, Sluyter R, Dao-Ung LP, Gu BJ, Wiley JS. (2005) A 5' intronic splice site polymorphism leads to a null allele of the P2X7 gene in 1-2% of the Caucasian population. FEBS Lett.579 (12): 2675-8. [PMID:15862308]

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Patrizia Pellegatti, Francesco Di Virgilio, John A. Peters.
P2X receptors: P2X7. Last modified on 22/08/2017. Accessed on 24/09/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=484.