5-BDBD 是选择性P2X4受体拮抗剂，抑制 rP2X4R 介导的电流，IC50为0.75μM。它可完全阻断硝酸甘油诱导的基础性和急性痛觉过敏。

5-BDBD is a potent and selective P2X4 receptor antagonist. 5-BDBD inhibits rP2X4R-mediated currents with an IC50 of 0.75 μM. 5-BDBD completely blocked the basal and acute hyperalgesia induced by NTG.

5-BDBD could be specifically used to discriminate between P2X1R, P2X2aR, P2X2bR, P2X3R, P2X4R, and P2X7R[1]. 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].

Basal hyperalgesia induced by recurrent NTG injection was completely blocked by 5-BDBD[2].

5-BDBD (28 mg/kg; i.p.; daily for 9 days; male C57BL/6 mice) prevented NTG-induced mechanical hypersensitivity[2].

768404-03-1

C17H11BrN2O2

355.19

DMSO:60 mg/mL (168.92 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years