For research use only. Not for therapeutic Use.
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].
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].
5-BDBD (28 mg/kg; i.p.; daily for 9 days) can completely blocke the basal hyperalgesia induced by recurrent NTG injection[2].
| Catalog Number | I010785 |
| CAS Number | 768404-03-1 |
| Synonyms | 5-(3-bromophenyl)-1,3-dihydro-[1]benzofuro[3,2-e][1,4]diazepin-2-one |
| Molecular Formula | C17H11BrN2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H11BrN2O2/c18-11-5-3-4-10(8-11)15-17-16(20-14(21)9-19-15)12-6-1-2-7-13(12)22-17/h1-8H,9H2,(H,20,21) |
| InChIKey | NKYMVQPXXTZHSF-UHFFFAOYSA-N |
| SMILES | C1C(=O)NC2=C(C(=N1)C3=CC(=CC=C3)Br)OC4=CC=CC=C42 |
| Reference | [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. |
