Discovery of P2X 7 receptor-selective antagonists offers new insights into P2X 7 receptor function and indicates a role in chronic pain states

British Journal of Pharmacology

Volumn 151, Issue 5, 2007, Pages 571-579

  Donnelly Roberts, D L ^a   Jarvis, M F ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

A 438079; A 740003; Allodynia; AZ11645373; Calcium influx; IL 1 ; Inflammatory pain; Neuropathic pain; P2X 7 receptor; Purines; Yo Pro uptake

Indexed keywords

1 [N,O BIS(5 ISOQUINOLINESULFONYL) N METHYLTYROSYL] 4 PHENYLPIPERAZINE; 3 [1 (3' NITROBIPHENYL 4 YLOXY) 4 (PYRIDIN 4 YL)BUTAN 2 YL]THIAZOLIDINE 2,4 DIONE; A 317491; A 438079; A 740003; ADENOSINE TRIPHOSPHATE 2',3' DIALDEHYDE; AZ 11645373; CALCIUM; DECAVANADIC ACID; INTERLEUKIN 1BETA; PURINE P2X7 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; PYRIDOXAL PHOSPHATE 6 AZOPHENYL 2',4' DISULFONIC ACID; SURAMIN; UNCLASSIFIED DRUG; ADENOSINE TRIPHOSPHATE; DRUG DERIVATIVE; PURINE P2 RECEPTOR;

AGONIST; CALCIUM CELL LEVEL; CELL MEMBRANE; CENTRAL NERVOUS SYSTEM; CHRONIC PAIN; CYTOKINE RELEASE; CYTOLYSIS; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; GENE DISRUPTION; GLIA CELL; HUMAN; INFLAMMATION; MACROPHAGE; NEUROPATHIC PAIN; NOCICEPTION; NONHUMAN; PHENOTYPE; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN LOCALIZATION; RECEPTOR BLOCKING; REVIEW; SIGNAL TRANSDUCTION; THERAPY EFFECT; ANIMAL; CHRONIC DISEASE; DRUG ANTAGONISM; DRUG EFFECT; DRUG POTENTIATION; PAIN; PATHOPHYSIOLOGY; PHYSIOLOGY; RAT;

ADENOSINE TRIPHOSPHATE; ANIMALS; CHRONIC DISEASE; HUMANS; INFLAMMATION; PAIN; RATS; RECEPTORS, PURINERGIC P2; SIGNAL TRANSDUCTION;

EID: 34347333404     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707265     Document Type: Review

References (97)

1. 7 receptors. J Biol Chem 278: 37344-37351.
2. 7. J Leukocyte Biol 72: 222-232.
3. 7 receptor antagonists. Bioorg Med Chem Lett 13: 4043-4046.
4. Anderson CM, Nedergaard M (2006). Emerging challenges of assigning P2X(7) receptor function and immunoreactivity in neurons. Trends Neurosci 29: 257-262.
5. 7-like receptors depresses mossy fiber-CA3 synaptic transmission through p38 mitogen-activated protein kinase. J Neurosci 22: 5938-5945.
6. Barbe MT, Monyer H, Bruzzone R (2006). Cell-cell communication beyond connexins: the pannexin channels. Physiol 21: 103-114.
7. 7 receptor antagonists. Bioorg Med Chem Lett 13: 4047-4050.
8. Beigi RD, Kertesy SB, Aquilina G, Dubyak GR (2003). Oxidized ATP (oATP) attenuates proinflammatory signaling via P2 receptor-independent mechanisms. Br J Pharmacol 140: 507-519.
9. Bianchi BR, Lynch KJ, Touma E, Niforatos W, Burgard EC, Alexander KM et al. (1999). Pharmacological characterization of recombinant human and rat P2X receptor subtypes. Eur J Pharmacol 376: 127-138.
10. Bianchi M, Dib B, Panerai AE (1998). Interleukin-1 and nociception in the rat. J Neurosci Res 53: 645-650.
11. 7 receptors activate protein kinase D and p42/p44 mitogen-activated protein kinase (MAPK) downstream of protein kinase C. Biochem J 366: 745-755.
12. Burnstock G (2006). Pathophysiology and therapeutic potential of purinergic signaling. Pharmacol Rev 58: 58-78.
13. 7 receptor of human leukemic lymphocytes. J. Immunol 175: 82-89.
14. Carter AB, Tephly LA, Hunnunghake GW (2001). The absence of activator protein1-dependent gene expression in THP-1 macrophages stimulated with phorbol esters is due to lack of p38 mitogen-activate protein kinase activation. J Biol Chem 276: 33826-33832.
15. 7 receptor channels. J Neurosci 22: 3061-3069.
16. Chessell IP, Grahames CBA, Michel AD, Humphrey PPA (2001). Dynamics of P2X7 receptor pore dilation: pharmacological and functional consequences. Drug Dev Res 53: 60-65.
17. 7 purinoceptor gene abolishes chronic inflammatory and neuropathic pain. Pain 114: 386-396.
18. 7 receptor. Neuropharmacology 36: 1277-1283.
19. 7 antagonist, oxidized ATP, in arthritic rats. Neurosci Lett 327: 87-90.
20. 7 ATP receptor inhibitor, oxidized ATP. Arthritis Rheum 46: 3378-3385.
21. 7 contains multiple protein- and lipid-interaction motifs including a potential binding site for bacterial lipopolysaccharide. J Immunol 167: 1871-1876.
22. 7 receptor in the immune system. In: Abbracchio MP and Williams M (eds). Purinergic and Pyrimidinergic Signalling. Springer Verlag: Heidelberg, GR, pp 355-373.
23. 7 receptor is not the only target. Br J Pharmacol 140: 441-443.
24. 7R)-induced pore formation in human THP-1 cells. J Pharmacol Exp Ther 308: 1053-1061.
25. Egan TM, Samways DSK, Li Z (2006). Biophysics of P2X Receptors. Eur J Physiol 452: 501-512.
26. Elssner A, Duncan M, Gavrillin M, Wewers MD (2004). A novel P2X7 receptor activator, the human cathelicidin-derived peptide LL37, induces IL-1β processing and release. J Immunol 172: 4987-4994.
27. Evans RJ, Lewis C, Buell G, Vlaera S, North RA, Surprenant A (1995). Pharmacological characterization of heterologously expressed ATP-gated cation channels (P2X purinoceptors). Mol Pharmacol 48: 178-183.
28. 7 receptor? Am J Physiol Cell Physiol 288: C260-C271.
29. Fernando SL, Saunders BM, Sluyter R, Skarratt KK, Golbberg H, Marks GB et al. (2007). A polymorphism in the P2X7 gene increases susceptibility to extrapulmonary tuberculosis. Am J Respir Crit Care Med 175: 360-366.
30. Ferrari D, Villalba M, Chiozzi P, Falzoni S, Ricciardi-Castagnoli P, DiVirgilio F (1996). Mouse microglial cells express a plasma membrane pore gated by extracellular ATP. J. Immunol 156: 1531-1539.
31. Ferrari D, Wesselborg S, Bauer M, Schulze-Osthoff K (1997). Extracellular ATP activates transcription factor NF-[kappa]B through the P2Z purinoreceptor by selectively targeting NF-[kappa]B. J Cell Biol. 139: 1635-1643.
32. Ferrari D, Pizzirani C, Adinolfi E, Lemoli RM, Curti A, Idzko M et al. (2006). The P2X7 receptor: a key player in IL-1 processing and release. J Immunol 176: 3877-3883.
33. Fields RD, Burnstock G (2006). Purinergic signaling in neuron-glia interactions. Nature Review 7: 423-436.
34. Fonfria E, Chambers LJ, Demont EH, Roman SA, Skaper SD, Michel AD (2005). Species and temperature dependent effects of a novel P2X7 receptor antagonist on recombinant and native P2X7 receptors. Soc Neurosci Abstr no. 958.1.
35. Z-receptor of human lymphocytes. Br J Pharmacol 120: 1483-1490.
36. 7 receptor-mediated ERK1/2 phosphorylation in human astrocytoma cells. Am J Physiol Cell Physiol 284: C571-C581.
37. Gever JR, Cockayne DA, Dillon MP, Burnstock G, Ford APDW (2006). Pharmacology of P2X channels. Eur J Physiol 452: 513-537.
38. Grahames GBA, Michel AD, Chessell IP, Humpreys PPA (1999). Pharmacological characerization of ATP-and LPS-induced IL-1β release in human monoctyes. Br J Pharmacol 127: 1915-1921.
39. Gu BJ, Zhang WY, Bendall LJ, Chessell IP, Buell GN, Wiley JS. (2000). Expression of P2X7 purinoceptors on human lymphocytes and monoctyes: evidence for nonfunctional P2X7 receptors. Am J Physiol 279: C1189-C1197.
40. Honore P, Wade CL, Zhong C, Harris RR, Wu C, Ghayur T et al. (2006a). Interleukin-1αβ gene-deficient mice show reduced nociceptive sensitivity in models of inflammatory and neuropathic pain but not post-operative pain. Behav Brain Res 167: 355-364.
41. Honore PM, Donnelly-Roberts D, Namovic M, Hsieh G, Zhu C, Mikusa J et al. (2006b). 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: 1376-1385.
42. Horai R, Saijo S, Tanioka H, Nakae S, Sudo K, Okahara A et al. (2000). Development of chronic inflammatory arthropathy resembling rheumatoid arthritis in interleukin 1 receptor antagonist-deficient mice. J Exp Med 191: 313-320.
43. 7 nucleotide receptor and associated phospholipase D activity by lipopolysaccharide and IFN-γ in the human THP-1 monocytic cell line. J Immunol 157: 5627-5637.
44. 7 nucelotide receptor: high selectivity for the human versus rat receptor. Mol Pharmacol 54: 22-32.
45. 4. J Pharmacol Sci 94: 112-114.
46. Jacobson KA, Jarvis MF, Williams M (2002). Perspective: purine and pyrimidine. (P2) receptors as drug targets. J Med Chem 45: 4057-4093.
47. 2/3 receptors, reduces chronic inflammatory and neuropathic pain in rats. Proc Natl Acad Sci USA 99: 17179-17184.
48. 3 homomeric and heteromeric channels to acute and chronic pain. Expert Opin Ther Targets 7: 513-522.
49. 7 receptors. Mol Pharmacol 58: 82-88.
50. Jiang LH, Rassendren F, MacKenzie AB, Zhang YH, Surprenant A, North RA (2005). N-methyl-D-glucamine and propidium dyes utilize different permeation pathways at rat P2X7 receptors. Am J Physiol Cell Physiol 289: C1295-C1302.
51. + release. Am J Cell Physiol 286: C1100-C1108.
52. Khakh BS, Bao XR, Labarca C, Lester HA (1999). Neuronal P2X transmitter-gated cation channels change their ion selectivity in seconds. Nature Neurosci 2: 322-330.
53. Khakh BS, North RA (2006). P2X receptors as cell-surface ATP sensors in health and disease. Nature 442: 527-532.
54. 7 receptor signaling complex. EMBO J 20: 6347-6358.
55. 7 receptor alters leukocyte function and attenuates an inflammatory response. J Immunol 168: 6436-6445.
56. Lakshmi S, Joshi PG (2005). Co-activation of P2Y2 receptor and TRPV channel by ATP: implications for ATP induced pain. Cell Mol Neurobiol 25: 819-832.
57. 7 antagonist. Soc Neurosci Abstr no. 958.2.
58. Locovei S, Scemes E, Qiu F, Spray DC, Dahl G (2007). Pannexin1 is part of the pore forming unit of the P2X(7) receptor death complex. FEBS Lett 581: 483-488.
59. Lowe PN, Beechey RB (1982). Interactions between the mitochondrial adenosinetriphosphatase and periodate-oxidized adenosine 5′-triphosphate, an affinity label for adenosine 5′-triphosphate binding sites. Biochemistry 21: 4073-4082.
60. MacKenzie A, Wilson HL, Kiss-Tosh E, Dower SK, North RA, Surprenant A (2001). Rapid secretion of interleukin-1β by microvesicle shedding. Immunity 8: 825-835.
61. Maier SF, Wietelak EP, Martin D, Watkins LR (1993). Interleukin-1 mediates the behavioral hyperalgesia produced by lithium chloride and endotoxin. Brain Res 623: 321-324.
62. 7 receptors. Br J Pharmacol 534: 19-26.
63. 7 receptor function. Br J Pharmacol 149: 948-957.
64. 7-associated pore or channel formation. Br J Pharmacol 147: 324-334.
65. Murgia M, Hanau S, Pizzo P, Rippa M, Di Virgilio F (1993). Oxidized ATP. An irreversible inhibitor of the macrophage purinergic P2Z receptor. J Biol Chem 268: 8199-81203.
66. 7 antagonists. J Med Chem 49: 3659-3666.
67. North AR (2002). Molecular physiology of P2X receptors. Physiol Rev 82: 1013-1067.
68. Ono K, Han J (2000). The p38 signal transduction pathway: activation and function. Cell Signal 12: 1-13.
69. 7-like receptor activation in astrocytes increases chemokine monocyte chemoattractant protein-1 expression via mitogen-activated protein kinase. J Neurosci 21: 7135-7142.
70. 7-receptors activation in Mueller glial cells from the human retina. J Neurosci 20: 5965-5972.
71. 7 mediates superoxide production in primary microglia and is up-regulated in a transgenic mouse model of Alzheimer's disease. J Biol Chem 278: 13309-13317.
72. 7 receptor. EMBO J 25: 5071-5082.
73. Perregaux DG, Gabel CA (1994). Interleukin-1β maturation and release in response to ATP and nigericin. J Biol Chem 269: 15195-15203.
74. Perregaux DG, McNiff P, Laliberte R, Conklyn M, Gabel CA (2000). ATP acts as an agonist to promote stimulus-induced secretion of IL-1β and IL-18 in Human Blood. J Immunol 165: 4615-4623.
75. 7 receptor involvement. Drug Dev Res 53: 83-90.
76. 7: cloning and expression of a human cDNA. J Biol Chem 272: 5482-5486.
77. Rassendren F, Buell GN, Newbolt A, North RA, Surprenant A (1997b). Identification of amino acid residues contributing to the pore of a P2X receptor. EMBO J 16: 3446-3454.
78. Safieh-Garabedian B, Poole S, Allchorne A, Winter J, Woolf CJ (1995). Contribution of interleukin-1 to the inflammation-induced increase in nerve growth factor levels and inflammatory hyperalgesia. Br J Pharmacol 115: 1265-1275.
79. Samad TA, Moore KA, Sapirstein A, Billet S, Allchorne A, Poole S et al. (2001). Interleukin-1beta-mediated induction of Cox-2 in the CNS contributes to inflammatory pain hypersensitivity. Nature 410: 471-475.
80. Sanz JM, DiVirgilio F (2000). Kinetics and mechanism of ATP-dependent IL-1β release from microglia cells. J. Immunol 164: 4893-4898.
81. 7-like cytolytic pore in human skin fibroblasts. Am J Physiol Cell Physiol 277: C755-C765.
82. 7-independent mechanism. J Immunol 163: 558-561.
83. 7 receptor expression in rodent brain. J Neurosci 24: 6307-6314.
84. Solle M, Labasi J, Perregaux DG, Stam E, Petrushova N, Koller BH et al. (2001). Altered cytokine production in mice lacking P2X7 receptors. J Biol Chem 276: 125-132.
85. Sommer C, Petrausch S, Lindenlaub T, Toyka K (1999). Neutralizing antibodies to interleukin1-receptor reduce pain-associated behavior in mice with experimental neuropathy. Neurosci Lett 270: 25-28.
86. 7 receptors, AZ11645373. Br J Pharmacol 149: 880-887.
87. Surprenant A, Rassendren F, Kawashima E, North RA, Buell G (1996). The Cytolytic P2z receptor for extracellular ATP identified as a P2X receptor (P2X7). Science 272: 735-738.
88. Tominaga M, Wada M, Masu M (2001). Potentiation of capsaicin receptor activity by metabotropic ATP receptors as a possible mechanism for ATP-evoked pain and hyperalgesia. Proc Natl Acad Sci USA 98: 6951-6956.
89. Touzani O, Boutin H, LeFeurve R, Parker L, Miller A, Luheshi G et al. (2002). Interleukin-1 influences ischemic brain damage in the mouse independently of the interleukin-1 type 1 receptor. J Neurosci 22: 38-43.
90. 4 receptors induced in spinal microglia gate tactile allodynia after nerve injury. Nature 424: 778-783.
91. 7 receptor-dependent blebbing and the activation of Rho-effector kinases, caspases, and IL-1 release. J Immunol 170: 5728-5738.
92. 7 receptor. Nature Neurosci 2: 315-321.
93. 7 receptor gene and chronic lymphocytic leukemia: a molecular study. Lancet 359: 1114-1119.
94. Wiley JS, Dao-Ung LP, Li C, Shemon AN, Gu BJ, Smart ML et al. (2003). An Ile-568 to Asn polymorphism prevents normal trafficking and function of the human P2X7 receptor. J Biol Chem 278: 17108-17113.
95. Wolf G, Yirmiya R, Goshen I, Iverfeldt K, Holmlund L, Takeda K et al. (2004). Impairment of interleukin-1 (IL-1) signaling reduces basal pain sensitivity in mice: genetic, pharmacological and developmental aspects. Pain 104: 471-480.
96. Woolf CJ, Allchorne A, Safieh-Garabedian B, Poole S (1997). Cytokines, nerve growth factor and inflammatory hyperalgesia: the contribution of tumour necrosis factor alpha. Br J Pharmacol 121: 417-424.
97. 7 receptors in non-neuronal cells of rat dorsal root ganglion. Brain Res 1052: 63-70.