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Novel P2X7 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2003The 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 +14 more
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Trends in Cell Biology, 2018
ATP, which is released under pathological conditions and is considered a damage-associated molecular pattern (DAMP), activates P2X7 receptors (P2X7Rs), trimeric plasma membrane ion channels selective for small cations. P2X7Rs are partners in NOD-like receptor containing a pyrin (NLRP3) inflammasome activation and promoters of tumor cell growth.
Di Virgilio, Francesco +2 more
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ATP, which is released under pathological conditions and is considered a damage-associated molecular pattern (DAMP), activates P2X7 receptors (P2X7Rs), trimeric plasma membrane ion channels selective for small cations. P2X7Rs are partners in NOD-like receptor containing a pyrin (NLRP3) inflammasome activation and promoters of tumor cell growth.
Di Virgilio, Francesco +2 more
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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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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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P2X7 A1513 polymorphisms and tuberculosis susceptibility
Respirology, 2011[Extract] It is interesting that two meta-analyses ofP2X7A1513C and tuberculosis susceptibility have been published in close succession and produce conflicting results.1,2 Because the meta-analyses appear to have been produced simultaneously, neither author has been able to comment on the other; accordingly, it is worth reflecting on the possible ...
Denholm, Justin T., McBryde, Emma S.
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Tissue distribution of the P2X7 receptor
Neuropharmacology, 1997The 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 +5 more
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Molecular Probes for P2X7 Receptor Studies
Current Medicinal Chemistry, 2007The 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 +2 more
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Effects of antidepressants on P2X7 receptors
Psychiatry Research, 2016Antidepressants 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 +4 more
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Analysis of P2X7-Induced Neuronal Branching
2022P2X7 receptors regulate different aspects of neuronal development, including neurogenesis, dendritic outgrowth, and axonal elongation. Primary neuronal culture is a widely used model system in neuroscience as it enables to study molecular and cellular events caused by the activation of different ion channels, receptors, and transporters under ...
Paula, Mut-Arbona, Beáta, Sperlágh
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Cubyl amides: Novel P2X7 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2008Polycyclic 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 +4 more
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P2X7 receptors in the nervous system
Progress in Neurobiology, 2006P2X(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 +3 more
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