Chemical Name: 5-(3-Bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one
Biological Activity5-BDBD is a potent and selective P2X4 receptor antagonist. Blocks P2X4-mediated currents in Chinese hamster ovary cells (IC50 = 0.50 μM). Exhibits no significant antagonist effects at other P2X receptors. Reduces long-term potentiation (LTP) in rat hippocampal slices.
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Cell-autonomous regulation of hematopoietic stem cell cycling activity by ATP.
Casati et al.
Cell Death Differ., 2011;18:396
Painful purinergic receptors.
Donnelly-Roberts et al.
Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor.
Coddou et al.
Neurosci Lett., 2018;
Citations for 5-BDBD
The citations listed below are publications that use Tocris products. Selected citations for 5-BDBD include:
17 Citations: Showing 1 - 10
Extracellular ATP Increases Glucose Metabolism in Skeletal Muscle Cells in a P2 Receptor Dependent Manner but Does Not Contribute to Palmitate-Induced Insulin Resistance.
Authors: Miguel Cruz & Beall
Front Physiol 2020;11
Ginsenosides Act As Positive Modulators of P2X4 Receptors.
Authors: Dhuna Et al.
Mol Pharmacol 2019;95:210
Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis.
Authors: Zumerle Et al.
Cell Rep 2019;27:1
Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage.
Authors: Uderhardt Et al.
Relative Role of Akt, ERK and CREB in Alcohol-Induced Microglia P2X4R Receptor Expression.
Authors: Gofman Et al.
Alcohol Alcohol 2016;51:647
Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense.
Authors: Ledderose Et al.
J Infect Dis 2016;213:456
Effect of P2X4R on airway inflammation and airway remodeling in allergic airway challenge in mice.
Authors: Chen Et al.
Mol Med Rep 2016;13:697
Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α.
Authors: Mascanfroni Et al.
Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors.
Authors: Kawano Et al.
PLoS One 2015;10:e0127919
A critical role for pannexin-1 in activation of innate immune cells of the choroid plexus.
Authors: Maslieieva and Thompson
Channels (Austin) 2014;8:131
Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium.
Authors: Shabir Et al.
Nat Med 2013;305:F396
Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.
Authors: Ilatovskaya Et al.
Am J Physiol Cell Physiol 2013;305:C1050
Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7.
Authors: Vergani Et al.
J Biol Chem 2013;127:463
Extracellular ATP exerts opposite effects on activated and regulatory CD4+ T cells via purinergic P2 receptor activation.
Authors: Trabanelli Et al.
J Immunol 2012;189:1303
Positive allosteric modulation by iverm. of human but not murine P2X7 receptors.
Authors: Nörenberg Et al.
Br J Pharmacol 2012;167:48
Functional expression of P2X4 receptor in capillary endothelial cells of the cochlear spiral ligament and its role in regulating the capillary diameter.
Authors: Wu Et al.
Am J Physiol Heart Circ Physiol 2011;301:H69
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DMSO dilution 10 μM