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768404-03-1

768404-03-1 structure
768404-03-1 structure
  • Name: 5-BDBD
  • Chemical Name: 5-(3-bromophenyl)-1,3-dihydro-[1]benzofuro[3,2-e][1,4]diazepin-2-one
  • CAS Number: 768404-03-1
  • Molecular Formula: C17H11BrN2O2
  • Molecular Weight: 355.18500
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
  • Create Date: 2016-09-23 21:02:50
  • Modify Date: 2024-01-11 15:42:25
  • 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].

Name 5-(3-bromophenyl)-1,3-dihydro-[1]benzofuro[3,2-e][1,4]diazepin-2-one
Synonyms 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
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
GHS07
Signal Word Warning
Hazard Statements H302
RIDADR NONH for all modes of transport