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Volumn 27, Issue 3, 2017, Pages 257-267

P2X7 receptor antagonists: a patent review (2010–2015)

Author keywords

IL 1 ; ion channel; P2X7 receptor; Purinergic receptor

Indexed keywords

BIOLOGICAL PRODUCT; PURINERGIC P2X7 RECEPTOR; PURINERGIC P2X7 RECEPTOR ANTAGONIST; PURINERGIC P2Y RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG; PURINERGIC P2X RECEPTOR ANTAGONIST;

EID: 85011945260     PISSN: 13543776     EISSN: 17447674     Source Type: Journal    
DOI: 10.1080/13543776.2017.1246538     Document Type: Review
Times cited : (80)

References (100)
  • 2
    • 0031754497 scopus 로고    scopus 로고
    • Receptors for purines and pyrimidines
    • Ralevic V, Burnstock G. Receptors for purines and pyrimidines. Pharmacol Rev. 1998;50:413–492.
    • (1998) Pharmacol Rev , vol.50 , pp. 413-492
    • Ralevic, V.1    Burnstock, G.2
  • 3
    • 0029665112 scopus 로고    scopus 로고
    • The cytolytic P2Z receptor for extracellular ATP identified as a P2X receptor (P2X7)
    • Surprenant A, Rassendren F, Kawashima E, et al. The cytolytic P2Z receptor for extracellular ATP identified as a P2X receptor (P2X7). Science. 1996;272(5262):735–738.
    • (1996) Science , vol.272 , Issue.5262 , pp. 735-738
    • Surprenant, A.1    Rassendren, F.2    Kawashima, E.3
  • 4
    • 39149105285 scopus 로고    scopus 로고
    • Cellular localization of P2X7 receptor mRNA in the rat brain
    • Yu Y, Ugawa S, Ueda T, et al. Cellular localization of P2X7 receptor mRNA in the rat brain. Brain Res. 2008;1194:45–55.
    • (2008) Brain Res , vol.1194 , pp. 45-55
    • Yu, Y.1    Ugawa, S.2    Ueda, T.3
  • 5
    • 0030609068 scopus 로고    scopus 로고
    • Tissue distribution of the P2X7 receptor
    • Collo G, Neidhart S, Kawashima E, et al. Tissue distribution of the P2X7 receptor. Neuropharmacology. 1997;36(9):1277–1283.
    • (1997) Neuropharmacology , vol.36 , Issue.9 , pp. 1277-1283
    • Collo, G.1    Neidhart, S.2    Kawashima, E.3
  • 6
    • 0035881559 scopus 로고    scopus 로고
    • Cutting edge: the nucleotide receptor P2X7 contains multiple protein- and lipid-interaction motifs including a potential binding site for bacterial lipopolysaccharide
    • Denlinger LC, Fisette PL, Sommer JA, et al. Cutting edge:the nucleotide receptor P2X7 contains multiple protein- and lipid-interaction motifs including a potential binding site for bacterial lipopolysaccharide. J Immunol. 2001;167(4):1871–1876.
    • (2001) Immunol , vol.167 , Issue.4 , pp. 1871-1876
    • Denlinger, L.C.1    Fisette, P.L.2    Sommer, J.A.3
  • 8
    • 67949117176 scopus 로고    scopus 로고
    • Crystal structure of the ATP-gated P2X(4) ion channel in the closed state
    • Kawate T, Michel JC, Birdsong WT, et al. Crystal structure of the ATP-gated P2X(4) ion channel in the closed state. Nature. 2009;460(7255):592–598.
    • (2009) Nature , vol.460 , Issue.7255 , pp. 592-598
    • Kawate, T.1    Michel, J.C.2    Birdsong, W.T.3
  • 9
    • 84860785529 scopus 로고    scopus 로고
    • Molecular mechanism of ATP binding and ion channel activation in P2X receptors
    • Hattori M, Gouaux E. Molecular mechanism of ATP binding and ion channel activation in P2X receptors. Nature. 2012;485(7397):207–213.• The two articles reported the first crystal structure of zP2X4 receptor, which suggested the gating mechanism of the ion channel through binding of the natural agonist, ATP.
    • (2012) Nature , vol.485 , Issue.7397 , pp. 207-213
    • Hattori, M.1    Gouaux, E.2
  • 10
    • 14444281120 scopus 로고    scopus 로고
    • Activation by P2X7 agonists of two phospholipases A2 (PLA2) in ductal cells of rat submandibular gland. Coupling of the calcium-independent PLA2 with kallikrein secretion
    • Alzola E, Pérez-Etxebarria A, et al. Activation by P2X7 agonists of two phospholipases A2 (PLA2) in ductal cells of rat submandibular gland. Coupling of the calcium-independent PLA2 with kallikrein secretion. J Biol Chem. 1998;273(46):30208–30217.
    • (1998) Biol Chem , vol.273 , Issue.46 , pp. 30208-30217
    • Alzola, E.1    Pérez-Etxebarria, A.2
  • 11
    • 0038107758 scopus 로고    scopus 로고
    • Regulation of phospholipase D by P2X7 receptors in submandibular ductal cells
    • Pochet S, Gómez-Muñoz A, Marino A, et al. Regulation of phospholipase D by P2X7 receptors in submandibular ductal cells. Cell Signal. 2003;15(10):927–935.
    • (2003) Cell Signal , vol.15 , Issue.10 , pp. 927-935
    • Pochet, S.1    Gómez-Muñoz, A.2    Marino, A.3
  • 12
    • 1942422683 scopus 로고    scopus 로고
    • Mechanisms of caspase-1 activation by P2X7 receptor-mediated K+ release
    • Kahlenberg JM, Dubyak GR. Mechanisms of caspase-1 activation by P2X7 receptor-mediated K+ release. Am J Physiol Cell Physiol. 2004;286(5):C1100–8.
    • (2004) Am J Physiol Cell Physiol , vol.286 , Issue.5 , pp. C1100-C1108
    • Kahlenberg, J.M.1    Dubyak, G.R.2
  • 13
    • 1342323323 scopus 로고    scopus 로고
    • Mitogen-activated protein kinase and caspase signaling pathways are required for P2X7 receptor (P2X7R)-induced pore formation in human THP-1 cells
    • Donnelly-Roberts DL, Namovic MT, Faltynek CR, et al. Mitogen-activated protein kinase and caspase signaling pathways are required for P2X7 receptor (P2X7R)-induced pore formation in human THP-1 cells. J Pharmacol Exp Ther. 2004;308(3):1053–1061.
    • (2004) Pharmacol Exp Ther , vol.308 , Issue.3 , pp. 1053-1061
    • Donnelly-Roberts, D.L.1    Namovic, M.T.2    Faltynek, C.R.3
  • 14
    • 3242673859 scopus 로고    scopus 로고
    • Extracellular nucleotides act through P2X7 receptors to activate NF-kappaB in osteoclasts
    • Korcok J, Raimundo LN, Ke HZ, et al. Extracellular nucleotides act through P2X7 receptors to activate NF-kappaB in osteoclasts. J Bone Miner Res. 2004;19(4):642–651.
    • (2004) Bone Miner Res , vol.19 , Issue.4 , pp. 642-651
    • Korcok, J.1    Raimundo, L.N.2    Ke, H.Z.3
  • 15
    • 0037851027 scopus 로고    scopus 로고
    • P2X7 receptor-dependent blebbing and the activation of rho-effector kinases, caspases, and IL-1 release
    • Verhoef PA, Estacion M, Schilling W, et al. P2X7 receptor-dependent blebbing and the activation of rho-effector kinases, caspases, and IL-1 release. J Immunol. 2003;170:5728–5738.
    • (2003) Immunol , vol.170 , pp. 5728-5738
    • Verhoef, P.A.1    Estacion, M.2    Schilling, W.3
  • 16
    • 33750473352 scopus 로고    scopus 로고
    • Pannexin-1 mediates large pore formation and interleukin-1beta release by the ATP-gated P2X7 receptor
    • Pelegrin P, Surprenant A. Pannexin-1 mediates large pore formation and interleukin-1beta release by the ATP-gated P2X7 receptor. Embo J. 2006;25:5071–5082.
    • (2006) Embo J , vol.25 , pp. 5071-5082
    • Pelegrin, P.1    Surprenant, A.2
  • 17
    • 33846438625 scopus 로고    scopus 로고
    • Pannexin 1 is part of the pore forming unit of the P2X7 receptor death complex
    • Locovei S, Scemes E, Qiu F, et al. Pannexin 1 is part of the pore forming unit of the P2X7 receptor death complex. FEBS Lett. 2007;581:483–488.
    • (2007) FEBS Lett , vol.581 , pp. 483-488
    • Locovei, S.1    Scemes, E.2    Qiu, F.3
  • 18
    • 53449102024 scopus 로고    scopus 로고
    • P2X7 receptor-pannexin 1 complex: pharmacology and signaling
    • Iglesias R, Locovei S, Roque A, et al. P2X7 receptor-pannexin 1 complex:pharmacology and signaling. Am J Physiol Cell Physiol. 2008;295(3):C752–C760.
    • (2008) Am J Physiol Cell Physiol , vol.295 , Issue.3 , pp. C752-C760
    • Iglesias, R.1    Locovei, S.2    Roque, A.3
  • 20
    • 67649991492 scopus 로고    scopus 로고
    • Targeting Interleukin-1 signaling in chronic inflammation: focus on P2X7 receptor and Pannexin-1
    • Pelegrin P. Targeting Interleukin-1 signaling in chronic inflammation:focus on P2X7 receptor and Pannexin-1. Drug News Perspect. 2008;21:24–33.
    • (2008) Drug News Perspect , vol.21 , pp. 24-33
    • Pelegrin, P.1
  • 21
    • 77952296338 scopus 로고    scopus 로고
    • Interleukin-1β (IL-1β) processing pathway
    • Weber A, Wasiliew P, Kracht M, et al. Interleukin-1β (IL-1β) processing pathway. Sci Signal. 2010;19:CM2.
    • (2010) Sci Signal , vol.19 , pp. CM2
    • Weber, A.1    Wasiliew, P.2    Kracht, M.3
  • 22
    • 33646072818 scopus 로고    scopus 로고
    • The P2X7 receptor: a key player in IL-1 processing and release
    • Ferrari D, Pizzirani C, Adinolfi E, et al. The P2X7 receptor:a key player in IL-1 processing and release. J Immunol. 2006;176:3877–3883.
    • (2006) Immunol , vol.176 , pp. 3877-3883
    • Ferrari, D.1    Pizzirani, C.2    Adinolfi, E.3
  • 23
    • 20144375454 scopus 로고    scopus 로고
    • Disruption of the P2X7 purinoceptor gene abolishes chronic inflammatory and neuropathic pain
    • Chessell IP, Hatcher JP, Bountra C, et al. Disruption of the P2X7 purinoceptor gene abolishes chronic inflammatory and neuropathic pain. Pain. 2005;114:386–396.
    • (2005) Pain , vol.114 , pp. 386-396
    • Chessell, I.P.1    Hatcher, J.P.2    Bountra, C.3
  • 24
    • 58549092549 scopus 로고    scopus 로고
    • Behavioral profile of P2X7 receptor knockout mice in animal models of depression and anxiety: relevance for neuropsychiatric disorders
    • Basso AM, Bratcher NA, Harris RR, et al. Behavioral profile of P2X7 receptor knockout mice in animal models of depression and anxiety:relevance for neuropsychiatric disorders. Behav Brain Res. 2009;198(1):83–90.
    • (2009) Behav Brain Res , vol.198 , Issue.1 , pp. 83-90
    • Basso, A.M.1    Bratcher, N.A.2    Harris, R.R.3
  • 25
    • 84871528843 scopus 로고    scopus 로고
    • The absence of P2X7 receptors (P2rx7) on non-haematopoietic cells leads to selective alteration in mood-related behaviour with dysregulated gene expression and stress reactivity in mice
    • Csölle C, Andó RD, Kittel Á, et al. The absence of P2X7 receptors (P2rx7) on non-haematopoietic cells leads to selective alteration in mood-related behaviour with dysregulated gene expression and stress reactivity in mice. Int J Neuropsychopharmacol. 2013;16(1):213–233.
    • (2013) Int J Neuropsychopharmacol , vol.16 , Issue.1 , pp. 213-233
    • Csölle, C.1    Andó, R.D.2    Kittel, Á.3
  • 26
    • 84888377850 scopus 로고    scopus 로고
    • Purinergic signalling and cancer
    • Burnstock G, Di Virgilio F. Purinergic signalling and cancer. Purinergic Signal. 2013;9(4):491–540.• This is the review article regarding the roles of P2X7 receptor with cancers.
    • (2013) Purinergic Signal , vol.9 , Issue.4 , pp. 491-540
    • Burnstock, G.1    Di Virgilio, F.2
  • 27
    • 78149373127 scopus 로고    scopus 로고
    • Targeting P2X₇ receptor inhibits the metastasis of murine P388D1 lymphoid neoplasm cells to lymph nodes
    • Ren S, Zhang Y, Wang Y, et al. Targeting P2X₇ receptor inhibits the metastasis of murine P388D1 lymphoid neoplasm cells to lymph nodes. Cell Biol Int. 2010;34(12):1205–1211.
    • (2010) Cell Biol Int , vol.34 , Issue.12 , pp. 1205-1211
    • Ren, S.1    Zhang, Y.2    Wang, Y.3
  • 28
    • 78149416375 scopus 로고    scopus 로고
    • Association of XIAP and P2X7 receptor expression with lymph node metastasis in papillary thyroid carcinoma
    • Gu LQ, Li FY, Zhao L, et al. Association of XIAP and P2X7 receptor expression with lymph node metastasis in papillary thyroid carcinoma. Endocrine. 2010;38(2):276–282.
    • (2010) Endocrine , vol.38 , Issue.2 , pp. 276-282
    • Gu, L.Q.1    Li, F.Y.2    Zhao, L.3
  • 29
    • 84880265647 scopus 로고    scopus 로고
    • Anthraquinone emodin inhibits human cancer cell invasiveness by antagonizing P2X7 receptors
    • Jelassi B, Anchelin M, Chamouton J, et al. Anthraquinone emodin inhibits human cancer cell invasiveness by antagonizing P2X7 receptors. Carcinogenesis. 2013;34(7):1487–1496.
    • (2013) Carcinogenesis , vol.34 , Issue.7 , pp. 1487-1496
    • Jelassi, B.1    Anchelin, M.2    Chamouton, J.3
  • 30
    • 84915756885 scopus 로고    scopus 로고
    • P2X7 mediates ATP-driven invasiveness in prostate cancer cells
    • Qiu Y, Li WH, Zhang H-Q, et al. P2X7 mediates ATP-driven invasiveness in prostate cancer cells. PLoS One. 2014;9(12):e114371.
    • (2014) PLoS One , vol.9 , Issue.12 , pp. e114371
    • Qiu, Y.1    Li, W.H.2    Zhang, H.-Q.3
  • 31
    • 84930015180 scopus 로고    scopus 로고
    • P2X7 receptor stimulates breast cancer cell invasion and migration via the AKT pathway
    • Xia J, Yu X, Tang L, et al. P2X7 receptor stimulates breast cancer cell invasion and migration via the AKT pathway. Oncol Rep. 2015;34(1):103–110.
    • (2015) Oncol Rep , vol.34 , Issue.1 , pp. 103-110
    • Xia, J.1    Yu, X.2    Tang, L.3
  • 32
    • 85011957773 scopus 로고    scopus 로고
    • Bethesda MD: National Center for Advancing Translational Sciences (NCATS), Available from
    • AZD9056. Bethesda MD:National Center for Advancing Translational Sciences (NCATS); 2011. Available from http://ncats.nih.gov/files/AZD9056.pdf
    • (2011)
  • 33
    • 84866105881 scopus 로고    scopus 로고
    • Clinical evaluation of the efficacy of the P2X7 purinergic receptor antagonist AZD9056 on the signs and symptoms of rheumatoid arthritis in patients with active disease despite treatment with methotrexate or sulphasalazine
    • Keystone EC, Wang MM, Layton M, et al. Clinical evaluation of the efficacy of the P2X7 purinergic receptor antagonist AZD9056 on the signs and symptoms of rheumatoid arthritis in patients with active disease despite treatment with methotrexate or sulphasalazine. Ann Rheum Dis. 2012;71(10):1630–1635.•• This article reported the results of phase IIa and IIb clinical studies of Astra Zeneca’s P2X7R targeted new drug candidate, AZD-9056 in the patients with rheumatoid arthritis.
    • (2012) Ann Rheum Dis , vol.71 , Issue.10 , pp. 1630-1635
    • Keystone, E.C.1    Wang, M.M.2    Layton, M.3
  • 34
    • 85011998175 scopus 로고    scopus 로고
    • Bethesda MD: National Center for Advancing Translational Sciences (NCATS), Available from
    • Pfizer CE-224535/P2X7 Receptor Antagonist. Bethesda MD:National Center for Advancing Translational Sciences (NCATS); 2011. Available from https://ncats.nih.gov/files/CE-224535.pdf
    • (2011)
  • 35
    • 84859456520 scopus 로고    scopus 로고
    • Efficacy and safety of CE-224,535, an antagonist of P2X7 receptor, in treatment of patients with rheumatoid arthritis inadequately controlled by methotrexate
    • Stock TC, Bloom BJ, Wei N, et al. Efficacy and safety of CE-224,535, an antagonist of P2X7 receptor, in treatment of patients with rheumatoid arthritis inadequately controlled by methotrexate. J Rheumatol. 2012;39(4):720–727.•• This article reported the results of phase IIa clinical study of Pfizer’s P2X7R targeted new drug candidate, CE-224,535 in the patients with rheumatoid arthritis.
    • (2012) Rheumatol , vol.39 , Issue.4 , pp. 720-727
    • Stock, T.C.1    Bloom, B.J.2    Wei, N.3
  • 36
    • 85012018080 scopus 로고    scopus 로고
    • United Kingdom: Evotec Ltd, Available from
    • Evotec grants exclusive rights on EVT 401 in China to conba pharmaceutical. United Kingdom:Evotec Ltd; 2012. Available from https://www.evotec.com/article/en/Press-releases/Evotec-grants-exclusive-rights-on-EVT-401-in-China-to-Conba-Pharmaceutical/2274
    • (2012) Evotec grants exclusive rights on EVT 401 in China to conba pharmaceutical
  • 37
    • 85012018075 scopus 로고    scopus 로고
    • United Kingdom: GlaxoSmithKline plc, Available from
    • Studies filtered by compound GSK1482160. United Kingdom:GlaxoSmithKline plc; 2009. Available from http://www.gsk-clinicalstudyregister.com/compounds/gsk1482160#ps
    • (2009)
  • 38
    • 85012018132 scopus 로고    scopus 로고
    • New York (NY): Torreya Insights, LLC, Available from
    • AFC-5128. New York (NY):Torreya Insights, LLC; 2011. Available from http://www.avarx.com/search/showOpportunityDetails?asset_id=1440
    • (2011)
  • 39
    • 85011944523 scopus 로고    scopus 로고
    • Imidazolidine carboxamide derivatives as P2X7 modulators
    • GSK. Imidazolidine carboxamide derivatives as P2X7 modulators. US20100075968 (2010)
    • (2010) US20100075968
  • 40
    • 85012023935 scopus 로고    scopus 로고
    • Thiadiazolidinedioxide P2X7 receptor antagonists
    • GSK. Thiadiazolidinedioxide P2X7 receptor antagonists. WO2011054947 (2011)
    • (2011) WO2011054947
  • 41
    • 85011958588 scopus 로고    scopus 로고
    • Pyrazole derivatives as P2X7 modulators
    • GSK. Pyrazole derivatives as P2X7 modulators. US20110046137 (2011)
    • (2011) US20110046137
  • 42
    • 85011944520 scopus 로고    scopus 로고
    • 4-benzoyl-1-substituted-piperazin-2-one derivatives as P2X7 modulators
    • GSK. 4-benzoyl-1-substituted-piperazin-2-one derivatives as P2X7 modulators. US20100311749 (2010)
    • (2010) US20100311749
  • 43
    • 85012010522 scopus 로고    scopus 로고
    • 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-A]pyrazine derivatives as P2X7 modulators
    • GSK. 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-A]pyrazine derivatives as P2X7 modulators. US20120157436 (2012)
    • (2012) US20120157436
  • 44
    • 85012018139 scopus 로고    scopus 로고
    • Quinoline derivatives 057
    • AstraZeneca. Quinoline derivatives 057. US8106073 (2012)
    • (2012) US8106073
  • 45
    • 85012010734 scopus 로고    scopus 로고
    • Compounds 679
    • AstraZeneca. Compounds 679. US7964616 (2011)
    • (2011) US7964616
  • 46
    • 85011963017 scopus 로고    scopus 로고
    • Dihydropyrimidone amides as P2X7 modulators
    • Roche. Dihydropyrimidone amides as P2X7 modulators. US20110028502 (2011)
    • (2011) US20110028502
  • 47
    • 85011965822 scopus 로고    scopus 로고
    • [1,2,4]triazolo[3,4-C][1,4]oxazines as P2X7 modulators
    • Roche. [1,2,4]triazolo[3,4-C][1,4]oxazines as P2X7 modulators. US20110071143 (2011)
    • (2011) US20110071143
  • 48
    • 85011976978 scopus 로고    scopus 로고
    • Amido compounds
    • Roche. Amido compounds. US20120149718 (2012)
    • (2012) US20120149718
  • 49
    • 85011979060 scopus 로고    scopus 로고
    • Isoindolyl compounds
    • Roche. Isoindolyl compounds. US20120157494 (2012)
    • (2012) US20120157494
  • 50
    • 85012003679 scopus 로고    scopus 로고
    • Quinoline or isoquinoline substituted P2X7 antagonists
    • Janssen Pharmaceutica. Quinoline or isoquinoline substituted P2X7 antagonists. US20110092481 (2011)
    • (2011) US20110092481
  • 51
    • 85011944589 scopus 로고    scopus 로고
    • 5,6,7,8,9,10-hexahydro-6,10-epimino[1,2,4]triazolo[4,3-a]azocines as P2X7 modulators
    • Janssen Pharmaceutica. 5,6,7,8,9,10-hexahydro-6,10-epimino[1,2,4]triazolo[4,3-a]azocines as P2X7 modulators. US20140275056 (2014)
    • (2014) US20140275056
  • 52
    • 85012018965 scopus 로고    scopus 로고
    • P2X7 modulators
    • Janssen Pharmaceutica. P2X7 modulators. US20140275120 (2014)
    • (2014) US20140275120
  • 53
    • 85011945280 scopus 로고    scopus 로고
    • [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
    • Janssen Pharmaceutica. [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators. US20140275096 (2014)
    • (2014) US20140275096
  • 54
    • 85011978176 scopus 로고    scopus 로고
    • Benzamide derivatives as P2X7 receptor antagonists
    • Actelion pharmaceuticals Ltd. Benzamide derivatives as P2X7 receptor antagonists. WO2012114268 (2012)
    • (2012) WO2012114268
  • 55
    • 85011978186 scopus 로고    scopus 로고
    • Heterocyclic amide derivatives as P2X7 receptor antagonists
    • Actelion pharmaceuticals Ltd. Heterocyclic amide derivatives as P2X7 receptor antagonists. US20140163035 (2014)
    • (2014) US20140163035
  • 56
    • 85011945283 scopus 로고    scopus 로고
    • Heterocyclic amide derivatives as P2X7 receptor antagonists
    • Actelion pharmaceuticals Ltd. Heterocyclic amide derivatives as P2X7 receptor antagonists. US20150025075 (2015)
    • (2015) US20150025075
  • 57
    • 85011979132 scopus 로고    scopus 로고
    • Indole carboxamide derivatives as P2X7 receptor antagonists
    • Actelion pharmaceuticals Ltd. Indole carboxamide derivatives as P2X7 receptor antagonists. WO2014097140 (2014)
    • (2014) WO2014097140
  • 58
    • 85011978184 scopus 로고    scopus 로고
    • Heteroaryl amide analogues
    • H. LUNDBECK A/S. Heteroaryl amide analogues. US20120190680 (2012)
    • (2012) US20120190680
  • 59
    • 85011978129 scopus 로고    scopus 로고
    • Heteroaryl amide derivatives
    • H. LUNDBECK A/S. Heteroaryl amide derivatives. US20120172366 (2013)
    • (2013) US20120172366
  • 60
    • 85011996323 scopus 로고    scopus 로고
    • Heteroaryl amide analogues as P2X7 antagonists
    • H. LUNDBECK A/S. Heteroaryl amide analogues as P2X7 antagonists. US8580812 (2013)
    • (2013) US8580812
  • 61
    • 85011958615 scopus 로고    scopus 로고
    • Benzamides
    • H. LUNDBECK A/S. Benzamides. WO2014057078 (2014)
    • (2014) WO2014057078
  • 62
    • 85011978132 scopus 로고    scopus 로고
    • N-(2-(cyclic amine)ethyl)benzamide derivatives as P2X7 inhibitors
    • H. LUNDBECK A/S. N-(2-(cyclic amine)ethyl)benzamide derivatives as P2X7 inhibitors. WO2014057080 (2014)
    • (2014) WO2014057080
  • 63
    • 85012003674 scopus 로고    scopus 로고
    • Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
    • Renovis, INC. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof. US20100184802 (2010)
    • (2010) US20100184802
  • 64
    • 85012010538 scopus 로고    scopus 로고
    • Novel compounds as P2X7 modulators and uses thereof
    • Renovis, INC. Novel compounds as P2X7 modulators and uses thereof. US20100022531 (2010)
    • (2010) US20100022531
  • 65
    • 85011944576 scopus 로고    scopus 로고
    • P2X7 receptor antagonists and methods of use
    • Abbott. P2X7 receptor antagonists and methods of use. US7709469 (2010)
    • (2010) US7709469
  • 66
    • 85011944569 scopus 로고    scopus 로고
    • Amino-tetrazoles analogues and methods of use
    • Abbott. Amino-tetrazoles analogues and methods of use. US7723367 (2010)
    • (2010) US7723367
  • 67
    • 85012003677 scopus 로고    scopus 로고
    • Pyridazinone compounds and P2X7 receptor inhibitors
    • Nissan chemical industries, Ltd. Pyridazinone compounds and P2X7 receptor inhibitors. US20100286390 (2010)
    • (2010) US20100286390
  • 68
    • 85011949375 scopus 로고    scopus 로고
    • Heterocyclic compounds as P2X7 ion channel blockers
    • Aventis Pharmaceuticals, Inc. Heterocyclic compounds as P2X7 ion channel blockers. US7741493 (2010)
    • (2010) US7741493
  • 69
    • 85011978139 scopus 로고    scopus 로고
    • Benzamide and heteroarylamide as P2X7 receptor antagonists
    • Pfizer Product Inc. Benzamide and heteroarylamide as P2X7 receptor antagonists. EP1448535 (2011)
    • (2011) EP1448535
  • 70
    • 85012023975 scopus 로고    scopus 로고
    • Triazolopyrazinones as P2X7 receptor antagonists
    • Schering corp. Triazolopyrazinones as P2X7 receptor antagonists. WO2012040048 (2012)
    • (2012) WO2012040048
  • 71
    • 85011978197 scopus 로고    scopus 로고
    • Substituted thiazole or oxazole P2X7 receptor antagonists
    • AXXAM S.P.A. Substituted thiazole or oxazole P2X7 receptor antagonists. WO2015118019 (2015)
    • (2015) WO2015118019
  • 72
    • 85011967461 scopus 로고    scopus 로고
    • Hybridomas producing antibodies against nonfunctional P2X7 receptor
    • Biosceptre International, Ltd. Hybridomas producing antibodies against nonfunctional P2X7 receptor. US20100105068 (2010)
    • (2010) US20100105068
  • 73
    • 85011945272 scopus 로고    scopus 로고
    • Combination therapy
    • Biosceptre International, Ltd. Combination therapy. US20150004179 (2015)
    • (2015) US20150004179
  • 74
    • 85011996343 scopus 로고    scopus 로고
    • P2X7 antagonists to treat affective disorders
    • Abbott. P2X7 antagonists to treat affective disorders. US20110269708 (2011)
    • (2011) US20110269708
  • 75
    • 85011998594 scopus 로고    scopus 로고
    • P2X7 antagonists as frontline or adjunctive treatment against status epilepticus
    • Royal College of Surgeons in Ireland. P2X7 antagonists as frontline or adjunctive treatment against status epilepticus. EP2604265 (2013)
    • (2013) EP2604265
  • 76
    • 85012018171 scopus 로고    scopus 로고
    • Imaging the central nervous system with purinergic P2X7 receptor binding agents
    • Jackson Alexander. Imaging the central nervous system with purinergic P2X7 receptor binding agents. US20120034165 (2012)
    • (2012) US20120034165
  • 77
    • 85012010760 scopus 로고    scopus 로고
    • Purine receptor inhibition as a therapeutic strategy in spinal cord and brain
    • Cornell Research Foundation, Inc. Purine receptor inhibition as a therapeutic strategy in spinal cord and brain. US7923448 (2011)
    • (2011) US7923448
  • 78
    • 85011945275 scopus 로고    scopus 로고
    • P2X7: Inhibition of epithelial cancers and papillomas
    • University Hospitals of Cleveland. P2X7:Inhibition of epithelial cancers and papillomas. US20140037576 (2014)
    • (2014) US20140037576
  • 79
    • 85011998591 scopus 로고    scopus 로고
    • Method for treatment of macular degeneration by modulating P2Y12 or P2X7 receptors
    • Claire Mitchell. Method for treatment of macular degeneration by modulating P2Y12 or P2X7 receptors. US20120264708 (2012)
    • (2012) US20120264708
  • 80
    • 85011998292 scopus 로고    scopus 로고
    • Therapies for disorders of the cornea and conjunctiva
    • Kaleko Michael. Therapies for disorders of the cornea and conjunctiva. US20140322193 (2014)
    • (2014) US20140322193
  • 81
    • 85011979130 scopus 로고    scopus 로고
    • Therapeutic agent for fatty liver disease containing P2X7 receptor inhibitory substance as active ingredient
    • Astellas Pharma Inc. Therapeutic agent for fatty liver disease containing P2X7 receptor inhibitory substance as active ingredient. WO2012036193 (2012)
    • (2012) WO2012036193
  • 82
    • 85011998621 scopus 로고    scopus 로고
    • P2X7 receptor agonist for use in preventing or treating kidney injury
    • UCL Business Plc. P2X7 receptor agonist for use in preventing or treating kidney injury. WO2014174282 (2014)
    • (2014) WO2014174282
  • 83
    • 85011978194 scopus 로고    scopus 로고
    • Use of P2X7 receptor antagonists to promote axonal growth and ramification
    • Miras Portugal. Use of P2X7 receptor antagonists to promote axonal growth and ramification. WO2010018280 (2010)
    • (2010) WO2010018280
  • 84
    • 84871151589 scopus 로고    scopus 로고
    • Pharmacokinetic and pharmacodynamic profiling of a P2X7 receptor allosteric modulator GSK1482160 in healthy human subjects
    • Ali Z, Laurijssens B, Ostenfeld T, et al. Pharmacokinetic and pharmacodynamic profiling of a P2X7 receptor allosteric modulator GSK1482160 in healthy human subjects. Br J Clin Pharmacol. 2013;75(1):197–207.
    • (2013) Br J Clin Pharmacol , vol.75 , Issue.1 , pp. 197-207
    • Ali, Z.1    Laurijssens, B.2    Ostenfeld, T.3
  • 85
    • 84942257551 scopus 로고    scopus 로고
    • Safety and efficacy of an oral inhibitor of the purinergic receptor P2X7 in adult patients with moderately to severely active crohn’s disease: a randomized placebo-controlled, double-blind, phase IIa study
    • Eser A, Colombel J-F, Rutgeerts P, et al. Safety and efficacy of an oral inhibitor of the purinergic receptor P2X7 in adult patients with moderately to severely active crohn’s disease:a randomized placebo-controlled, double-blind, phase IIa study. Inflamm Bowel Dis. 2015;21(10):2247–2253.•• This article reported the results of phase IIa clinical study of Astra Zeneca’s P2X7R targeted new drug candidate, AZD-9056 in the patients with Crohn’s disease.
    • (2015) Inflamm Bowel Dis , vol.21 , Issue.10 , pp. 2247-2253
    • Eser, A.1    Colombel, J.-F.2    Rutgeerts, P.3
  • 86
    • 84866990701 scopus 로고    scopus 로고
    • Extracellular ATP mediates mast cell-dependent intestinal inflammation through P2X7 purinoceptors
    • Kurashima Y, Amiya T, Nochi T, et al. Extracellular ATP mediates mast cell-dependent intestinal inflammation through P2X7 purinoceptors. Nat Commun. 2012;3:1034.• This article reported the roles of P2X7 receptor with intestinal inflammation in the patients with Crohn’s disease.
    • (2012) Nat Commun , vol.3 , pp. 1034
    • Kurashima, Y.1    Amiya, T.2    Nochi, T.3
  • 87
    • 84862777282 scopus 로고    scopus 로고
    • Genetically determined P2X7 receptor pore formation regulates variability in chronic pain sensitivity
    • Sorge RE, Trang T, Dorfman R, et al. Genetically determined P2X7 receptor pore formation regulates variability in chronic pain sensitivity. Nat Med. 2012;18(4):595–599.
    • (2012) Nat Med , vol.18 , Issue.4 , pp. 595-599
    • Sorge, R.E.1    Trang, T.2    Dorfman, R.3
  • 88
    • 84908373979 scopus 로고    scopus 로고
    • Over-expression of P2X7 receptors in spinal glial cells contributes to the development of chronic postsurgical pain induced by skin/muscle incision and retraction (SMIR) in rats
    • Ying YL, Wei XH, Xu X-B, et al. Over-expression of P2X7 receptors in spinal glial cells contributes to the development of chronic postsurgical pain induced by skin/muscle incision and retraction (SMIR) in rats. Exp Neurol. 2014;261:836–843.
    • (2014) Exp Neurol , vol.261 , pp. 836-843
    • Ying, Y.L.1    Wei, X.H.2    Xu, X.-B.3
  • 89
    • 84945436074 scopus 로고    scopus 로고
    • Interactions of pannexin 1 with NMDA and P2X7 receptors in central nervous system pathologies: Possible role on chronic pain
    • Bravo D, Maturana CJ, Pelissier T, et al. Interactions of pannexin 1 with NMDA and P2X7 receptors in central nervous system pathologies:Possible role on chronic pain. Pharmacol Res. 2015;101:86–93.
    • (2015) Pharmacol Res , vol.101 , pp. 86-93
    • Bravo, D.1    Maturana, C.J.2    Pelissier, T.3
  • 90
    • 77952746529 scopus 로고    scopus 로고
    • P2X7 receptor signaling pathway as a therapeutic target for neurodegenerative diseases
    • Takenouchi T, Sekiyama K, Sekigawa A, et al. P2X7 receptor signaling pathway as a therapeutic target for neurodegenerative diseases. Arch Immunol Ther Exp (Warsz). 2010;58(2):91–96.
    • (2010) Arch Immunol Ther Exp (Warsz) , vol.58 , Issue.2 , pp. 91-96
    • Takenouchi, T.1    Sekiyama, K.2    Sekigawa, A.3
  • 92
    • 84938983879 scopus 로고    scopus 로고
    • P2X purinoceptors as a link between hyperexcitability and neuroinflammation in status epilepticus
    • Henshall DC, Engel T. P2X purinoceptors as a link between hyperexcitability and neuroinflammation in status epilepticus. Epilepsy Behav. 2015;49:8–12.
    • (2015) Epilepsy Behav , vol.49 , pp. 8-12
    • Henshall, D.C.1    Engel, T.2
  • 93
    • 84955611614 scopus 로고    scopus 로고
    • Psychological stress activates the inflammasome via release of adenosine triphosphate and stimulation of the purinergic type 2x7 receptor
    • Iwata M, Ota KT, et al. Psychological stress activates the inflammasome via release of adenosine triphosphate and stimulation of the purinergic type 2x7 receptor. Biol Psychiatry. 2015;80(1):12–22.
    • (2015) Biol Psychiatry
    • Iwata, M.1    Ota, K.T.2
  • 94
    • 84930928841 scopus 로고    scopus 로고
    • Synthesis of [(11)C]GSK1482160 as a new PET agent for targeting P2X7 receptor
    • Gao M, Wang M, Green MA, et al. Synthesis of [(11)C]GSK1482160 as a new PET agent for targeting P2X7 receptor. Bioorg Med Chem Lett. 2015;25(9):1965–1970.
    • (2015) Bioorg Med Chem Lett , vol.25 , Issue.9 , pp. 1965-1970
    • Gao, M.1    Wang, M.2    Green, M.A.3
  • 95
    • 84876263632 scopus 로고    scopus 로고
    • Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists
    • Letavic MA, Lord B, Bischoff F, et al. Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists. ACS Med Chem Lett. 2013;4(4):419–422.
    • (2013) ACS Med Chem Lett , vol.4 , Issue.4 , pp. 419-422
    • Letavic, M.A.1    Lord, B.2    Bischoff, F.3
  • 96
    • 84952867693 scopus 로고    scopus 로고
    • A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334
    • Lord B, Ameriks MK, Wang Q, et al. A novel radioligand for the ATP-gated ion channel P2X7:[3H] JNJ-54232334. Eur J Pharmacol. 2015;765:551–559.
    • (2015) Eur J Pharmacol , vol.765 , pp. 551-559
    • Lord, B.1    Ameriks, M.K.2    Wang, Q.3
  • 97
    • 84934809021 scopus 로고    scopus 로고
    • Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists
    • Rudolph DA, Alcazar J, et al. Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists. Bioorg Med Chem Lett. 2015;25(16):3157–3163.
    • (2015) Bioorg Med Chem Lett , vol.25 , Issue.16 , pp. 3157-3163
    • Rudolph, D.A.1    Alcazar, J.2
  • 98
    • 84908409069 scopus 로고    scopus 로고
    • Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432
    • Lord B, Aluisio L, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014;351(3):628–641.
    • (2014) Pharmacol Exp Ther , vol.351 , Issue.3 , pp. 628-641
    • Lord, B.1    Aluisio, L.2
  • 99
    • 84966340408 scopus 로고    scopus 로고
    • Novel phenyl-substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists with robust target engagement in rat brain
    • Chrovian CC, Soyode-Johnson A, et al. Novel phenyl-substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists with robust target engagement in rat brain. ACS Chem Neurosci. 2016;7(4):490–497.
    • (2016) ACS Chem Neurosci , vol.7 , Issue.4 , pp. 490-497
    • Chrovian, C.C.1    Soyode-Johnson, A.2
  • 100
    • 84966318957 scopus 로고    scopus 로고
    • Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 antagonists
    • Ziff J, Rudolph DA, Stenne B, et al. Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 antagonists. ACS Chem Neurosci. 2016;7(4):498–504.
    • (2016) ACS Chem Neurosci , vol.7 , Issue.4 , pp. 498-504
    • Ziff, J.1    Rudolph, D.A.2    Stenne, B.3


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