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5-BDBD

5-BDBD用途

5-BDBD是一种有效的选择性P2X4受体拮抗剂,可抑制rP2X4R介导的电流,IC50为0.75μM。5-BDBD可完全阻断硝酸甘油(NTG)诱导的基础和急性痛觉过敏[1][2]。

5-BDBD名称

[ CAS 号 ]:
768404-03-1

[ 中文名 ]:
5-(3-溴苯基)-1,3-二氢-2H-苯并呋喃并[3,2-E] -1,4-二氮杂-2-酮

[ 英文名 ]:
5-BDBD

[英文别名 ]:

5-bdbd

5-BDBD生物活性

[ 描述 ]:

5-BDBD是一种有效的选择性P2X4受体拮抗剂,可抑制rP2X4R介导的电流,IC50为0.75μM。5-BDBD可完全阻断硝酸甘油(NTG)诱导的基础和急性痛觉过敏[1][2]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> P2X受体

研究领域 >> 神经疾病

[ 靶点 ]

I50: 0.75 μM (P2X4 receptor)

[体外研究]

5-BDBD以浓度依赖性方式抑制表达rP2X4R的HEK293细胞的10µM ATP诱导电流,IC50为0.75μM[1]。5-BDBD向右移动ATP浓度响应曲线,EC50为4.7至15.9μM[1]。5-BDBD可专门用于区分P2X1R、P2X2aR、P2X2bR、P2X3R、P2X4R和P2X7R[1]。

[体内研究]

5-BDBD(28 mg/kg；i.p；每日9天)可完全阻断反复注射NTG引起的基底痛过敏[2]。动物模型：雄性C57BL/6小鼠[2]剂量：28mg/kg给药：腹腔注射。；结果：预防了NTG诱导的机械性超敏反应。

[参考文献]

[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物理化学性质

[ 分子式 ]:
C₁₇H₁₁BrN₂O₂

[ 分子量 ]:
355.18500

[ 精确质量 ]:
354.00000

[ PSA ]:
58.09000

[ LogP ]:
3.50550

[ 储存条件 ]:
2-8°C，密封，干燥

5-BDBD安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危险品运输编码 ]:
NONH for all modes of transport

5-BDBD文献

Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors.

PLoS ONE 10 , e0127919, (2015)

Extracellular nucleotides, such as ATP, are released from cells in response to various stimuli and act as intercellular signaling molecules through activation of P2 receptors. Exposure to the ultravio...

Effect of P2X4R on airway inflammation and airway remodeling in allergic airway challenge in mice.

Mol. Med. Report. 13 , 697-704, (2015)

P2X4 receptor (P2X4R) is the most widely expressed subtype of the P2XRs in the purinergic receptor family. Adenosine triphosphate (ATP), a ligand for this receptor, has been implicated in the pathogen...

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