| Bioactivity | 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]. | ||||||||||||
| Target | I50: 0.75 μM (P2X4 receptor) | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | 5-BDBD | ||||||||||||
| CAS | 768404-03-1 | ||||||||||||
| Formula | C17H11BrN2O2 | ||||||||||||
| Molar Mass | 355.19 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
5-BDBD
CAS: 768404-03-1 F: C17H11BrN2O2 W: 355.19
5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-
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