5-BDBD

更新时间：2024-01-11 15:42:25

5-BDBD结构式	常用名	5-BDBD	英文名	5-BDBD
	CAS号	768404-03-1	分子量	355.18500
	密度	N/A	沸点	N/A
	分子式	C₁₇H₁₁BrN₂O₂	熔点	N/A
	MSDS	中文版美版	闪点	N/A
	符号	GHS07	信号词	Warning

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]。

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-(3-bromophenyl)-1,3-dihydro-[1]benzofuro[3,2-e][1,4]diazepin-2-one
英文别名	更多

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.

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

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

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PLoS ONE 10 , e0127919, (2015)

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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...

5-bdbd