Name | 5-(3-bromophenyl)-1,3-dihydro-[1]benzofuro[3,2-e][1,4]diazepin-2-one |
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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]. |
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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 |
Molecular Formula | C17H11BrN2O2 |
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Molecular Weight | 355.18500 |
Exact Mass | 354.00000 |
PSA | 58.09000 |
LogP | 3.50550 |