Catalog # Availability Size / Price Qty
5-BDBD | CAS No. 768404-03-1 | P2X Receptor Antagonists
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Description: Potent and selective P2X4 antagonist

Chemical Name: 5-(3-Bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one

Purity: ≥99%

Product Details
Citations (26)
Supplemental Products

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

Soluble to 100 mM in DMSO
Store at RT

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

  1. Cell-autonomous regulation of hematopoietic stem cell cycling activity by ATP.
    Casati et al.
    Cell Death Differ., 2011;18:396
  2. Painful purinergic receptors.
    Donnelly-Roberts et al.
    J.Pharmacol.Exp.Ther., 2008;324:409
  3. Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor.
    Coddou et al.
    Neurosci Lett., 2018;

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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

  1. Motoneuronal inflammasome activation triggers excessive neuroinflammation and impedes regeneration after sciatic nerve injury.
    Authors: László Et al.
    J Neuroinflammation  2022;19:68
  2. 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
  3. Characterization of purinergic receptor 2 signaling in podocytes from diabetic kidneys.
    Authors: Vladislav Et al.
    iScience  2021;24:102528
  4. 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
  5. 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
  6. Pharmacological and genetic characterisation of the canine P2X4 receptor.
    Authors: Belinda L Et al.
    Br J Pharmacol  2020;177:2812-2829
  7. 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
  8. Ginsenosides Act As Positive Modulators of P2X4 Receptors.
    Authors: Dhuna Et al.
    Mol Pharmacol  2019;95:210
  9. Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
    Authors: Dosch Et al.
    Elife  2019;8
  10. Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis.
    Authors: Zumerle Et al.
    Cell Rep  2019;27:1
  11. Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage.
    Authors: Uderhardt Et al.
    Cell  2019;177:541
  12. Keratinocytes mediate innocuous and noxious touch via ATP-P2X4 signaling.
    Authors: Aron M Et al.
    Elife  2018;7
  13. Relative Role of Akt, ERK and CREB in Alcohol-Induced Microglia P2X4R Receptor Expression.
    Authors: Gofman Et al.
    Alcohol Alcohol  2016;51:647
  14. 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
  15. Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense.
    Authors: Ledderose Et al.
    J Infect Dis  2016;213:456
  16. 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
  17. Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α.
    Authors: Mascanfroni Et al.
    Circulation  2015;21:638
  18. 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
  19. P2X4 receptor regulates alcohol-induced responses in microglia.
    Authors: Raghava Et al.
    J Neuroimmune Pharmacol  2014;9:668-78
  20. 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
  21. Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium.
    Authors: Shabir Et al.
    Nat Med  2013;305:F396
  22. 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
  23. Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7.
    Authors: Vergani Et al.
    J Biol Chem  2013;127:463
  24. 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
  25. Positive allosteric modulation by iverm. of human but not murine P2X7 receptors.
    Authors: Nörenberg Et al.
    Br J Pharmacol  2012;167:48
  26. 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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