5-BDBD

[Description]:

5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG)[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

Research Areas >> Neurological Disease

[Target]

I50: 0.75 μM (P2X4 receptor)

[In Vitro]

5-BDBD inhibits 10 µM ATP-induced currents of rP2X4R-expressing HEK293 cells in a concentration-dependent manner, with an IC50 of 0.75 μM[1]. 5-BDBD displaces rightward the ATP concentration-response curve, with an EC50 of 4.7 to 15.9 μM[1]. 5-BDBD could be specifically used to discriminate between P2X1R, P2X2aR, P2X2bR, P2X3R, P2X4R, and P2X7R[1].

[In Vivo]

5-BDBD (28 mg/kg; i.p.; daily for 9 days) can completely blocke the basal hyperalgesia induced by recurrent NTG injection[2]. Animal Model: Male C57BL/6 mice[2] Dosage: 28 mg/kg Administration: I.p.; daily for 9 days Result: Prevented NTG-induced mechanical hypersensitivity.

[References]

[1]. Coddou C, et al. Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor. Neurosci Lett. 2019;690:219-224.

[2]. Long T, et al. Microglia P2X4 receptor contributes to central sensitization following recurrent nitroglycerin stimulation. J Neuroinflammation. 2018;15(1):245. Published 2018 Aug 30.

[ Molecular Formula ]:
C₁₇H₁₁BrN₂O₂

[ Molecular Weight ]:
355.18500

[ Exact Mass ]:
354.00000

[ PSA ]:
58.09000

[ LogP ]:
3.50550

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors.

PLoS ONE 10 , e0127919, (2015)

Extracellular nucleotides, such as ATP, are released from cells in response to various stimuli and act as intercellular signaling molecules through activation of P2 receptors. Exposure to the ultravio...

Effect of P2X4R on airway inflammation and airway remodeling in allergic airway challenge in mice.

Mol. Med. Report. 13 , 697-704, (2015)

P2X4 receptor (P2X4R) is the most widely expressed subtype of the P2XRs in the purinergic receptor family. Adenosine triphosphate (ATP), a ligand for this receptor, has been implicated in the pathogen...

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