5-BDBD
Chemical Name: 5-(3-Bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one
Purity: ≥99%
Biological Activity
5-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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Electrical stimulation drives chondrogenesis of mesenchymal stem cells in the absence of exogenous growth factors
Sci Rep, 2016;6(0):39302. -
Extracellular ATP exerts opposite effects on activated and regulatory CD4+ T cells via purinergic P2 receptor activation.
J. Immunol., 2012;189(3):1303-10. -
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.
J.Pharmacol.Exp.Ther., 2008;324:409 -
Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor.
Coddou et al.
Neurosci Lett., 2018; -
Lipopolysaccharide suppresses T cells by generating extracellular ATP that impairs their mito-chondrial function via P2Y11 receptors
K Sueyoshi, C Ledderose, Y Shen, AH Lee, NI Shapiro, WG Junger
J. Biol. Chem., 2019;0(0):.
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Citations for 5-BDBD
The citations listed below are publications that use Tocris products. Selected citations for 5-BDBD include:
26 Citations: Showing 1 - 10
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Motoneuronal inflammasome activation triggers excessive neuroinflammation and impedes regeneration after sciatic nerve injury.
Authors: László Et al.
J Neuroinflammation 2022;19:68
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Modulation of P2X4 receptor activity by ivermectin and 5-BDBD has no effect on the development of ARPKD in PCK rats.
Authors: Vladislav Et al.
Physiol Rep 2022;10:e15510
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Characterization of purinergic receptor 2 signaling in podocytes from diabetic kidneys.
Authors: Vladislav Et al.
iScience 2021;24:102528
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Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells.
Authors: Timothy S Et al.
J Immunol 2021;207:1275-1287
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Astragalin Alleviates Neuropathic Pain by Suppressing P2X4-Mediated Signaling in the Dorsal Root Ganglia of Rats.
Authors: Rui Et al.
Front Neurosci 2021;14:570831
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Pharmacological and genetic characterisation of the canine P2X4 receptor.
Authors: Belinda L Et al.
Br J Pharmacol 2020;177:2812-2829
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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
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Ginsenosides Act As Positive Modulators of P2X4 Receptors.
Authors: Dhuna Et al.
Mol Pharmacol 2019;95:210
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Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Elife 2019;8
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Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis.
Authors: Zumerle Et al.
Cell Rep 2019;27:1
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Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage.
Authors: Uderhardt Et al.
Cell 2019;177:541
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Keratinocytes mediate innocuous and noxious touch via ATP-P2X4 signaling.
Authors: Aron M Et al.
Elife 2018;7
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Relative Role of Akt, ERK and CREB in Alcohol-Induced Microglia P2X4R Receptor Expression.
Authors: Gofman Et al.
Alcohol Alcohol 2016;51:647
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Purinergic and store-operated Ca(2+) signaling mechanisms in mesenchymal stem cells and their roles in ATP-induced stimulation of cell migration.
Authors: Peng Et al.
Stem Cells 2016;34:2102
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Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense.
Authors: Ledderose Et al.
J Infect Dis 2016;213:456
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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
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Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α.
Authors: Mascanfroni Et al.
Circulation 2015;21:638
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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
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P2X4 receptor regulates alcohol-induced responses in microglia.
Authors: Raghava Et al.
J Neuroimmune Pharmacol 2014;9:668-78
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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
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Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium.
Authors: Shabir Et al.
Nat Med 2013;305:F396
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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
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Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7.
Authors: Vergani Et al.
J Biol Chem 2013;127:463
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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
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Positive allosteric modulation by iverm. of human but not murine P2X7 receptors.
Authors: Nörenberg Et al.
Br J Pharmacol 2012;167:48
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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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