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The Purinergic P2X7 Receptor as a Target for Adjunctive Treatment for Drug-Refractory Epilepsy. [PDF]

Int J Mol Sci
Thakku Sivakumar D, Jain K, Alfehaid N, Wang Y, Teng X, Fischer W, Engel T.   +6 more
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Novel P2X7 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2003
The synthesis and pharmacological evaluation of a new series of potent P2X(7) receptor antagonists is disclosed. The compounds inhibit BzATP-mediated pore formation in THP-1 cells. The distribution of the P2X(7) receptor in inflammatory cells, most notably the macrophage, mast cell and lymphocyte, suggests that P2X(7) antagonists have a significant ...
L, Alcaraz, A, Baxter, J, Bent, K, Bowers, M, Braddock, D, Cladingboel, D, Donald, M, Fagura, M, Furber, C, Laurent, M, Lawson, M, Mortimore, M, McCormick, N, Roberts, M, Robertson   +14 more
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Tissue distribution of the P2X7 receptor

Neuropharmacology, 1997
The P2X7 receptor is a bifunctional molecule. The binding of ATP induces within milliseconds the opening of a channel selective for small cations, and within seconds a larger pore opens which allows permeation by molecules as large as propidium dyes (629 Da).
COLLO, Luigia Rinalda, NEIDHART S, KAWASHIMA E, KOSCO VILBOIS M, NORTH RA, BUELL G.   +5 more
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Molecular Probes for P2X7 Receptor Studies

Current Medicinal Chemistry, 2007
The ionotropic P2X7 receptor (P2X7R) has become the focus of intense research interest for a number of reasons: i) it is a cation selective ion channel that is modulated by extracellular ATP. Upon stimulation by high concentrations of ATP it generates a non-selective membrane pore which is permeable to hydrophilic molecules with molecular weight up to ...
Gunosewoyo, Hendra, Coster, Mark J, Kassiou, Michael   +2 more
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Effects of antidepressants on P2X7 receptors

Psychiatry Research, 2016
Antidepressants including paroxetine, fluoxetine and desipramine are commonly used for treating depression. P2×7 receptors are member of the P2X family. Recent studies indicate that these receptors may constitute a novel potential target for the treatment of depression. In the present study, we examined the action of these antidepressants on cloned rat
Wei, Wang, Zheng-Hua, Xiang, Chun-Lei, Jiang, Wei-Zhi, Liu, Zhi-Lei, Shang   +4 more
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The P2X7 Receptor

2017
The P2X7 receptor is a trimeric ion channel gated by extracellular adenosine 5'-triphosphate. The receptor is present on an increasing number of different cells types including stem, blood, glial, neural, ocular, bone, dental, exocrine, endothelial, muscle, renal and skin cells.
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Cubyl amides: Novel P2X7 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2008
Polycyclic amides 2 and 5-9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity.
Gunosewoyo, Hendra, Guo, Jun Liu, Bennett, Maxwell R, Coster, Mark J, Kassiou, Michael   +4 more
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P2X7 receptors in the nervous system

Progress in Neurobiology, 2006
P2X(7) receptors are ligand-gated ion channels, expressed as homo-oligomeric assemblies of individual subunits. They are widely distributed at immunocompetent cells of the central and peripheral nervous system and are believed to be primarily involved in host-defense reaction. However, a growing amount of evidence indicates that their signaling role in
Beáta, Sperlágh, E Sylvester, Vizi, Kerstin, Wirkner, Peter, Illes   +3 more
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P2X7 receptor antagonism: Implications in diabetic retinopathy

Biochemical Pharmacology, 2017
Diabetic retinopathy (DR) is the most frequent complication of diabetes and one of leading causes of blindness worldwide. Early phases of DR are characterized by retinal pericyte loss mainly related to concurrent inflammatory process. Recently, an important link between P2X7 receptor (P2X7R) and inflammation has been demonstrated indicating this ...
Platania C, Giurdanella G, Di Paola L, Leggio GM, Drago F, Salomone S, Bucolo C.   +6 more
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P2X7 Receptor as a Therapeutic Target

2016
P2X7 receptor is an ATP-gated cation channel that upon agonist interaction leads to cellular influx of Na(+) and Ca(2+) and efflux of K(+). P2X7 is expressed by a wide variety of cells and its activation mediates a large number of biological processes like inflammation, neuromodulation, cell death or cell proliferation and it has been associated to ...
DE MARCHI, Elena, ORIOLI, Elisa, Dal Ben, Diego, ADINOLFI, Elena   +3 more
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