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28434-74-4

28434-74-4结构式
28434-74-4结构式

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英文名 sodium,3-(butylamino)-4-phenoxy-5-sulfamoylbenzoate
英文别名 Sodium 3-(aminosulphonyl)-5-(butylamino)-4-phenoxybenzoate
Sodium 3-(butylamino)-4-phenoxy-5-sulfamoylbenzoate
Benzoic acid,3-(aminosulfonyl)-5-(butylamino)-4-phenoxy-,sodium salt (1:1)
SODIUM 3-(AMINOSULFONYL)-5-(BUTYLAMINO)-4-PHENOXYBENZOATE
Benzoic acid,3-(butylamino)-4-phenoxy-5-sulfamoyl-,monosodium salt (8CI)
EINECS 249-015-6
sodium bumetanide
Benzoicacid,3-(aminosulfonyl)-5-(butylamino)-4-phenoxy-,monosodium salt (9CI)
描述 布美他尼钠是一种高效的环状利尿剂,是一种钠钾氯协同转运(NKCC)阻滞剂。布美他尼钠是一种选择性NKCC1抑制剂,也抑制NKCC2,HNKCCC1a和HNKCCC2a的IC50s分别为0.68和4.0μM[1][2]。
相关类别
体外研究 布美他尼钠对NKCC的两种主要人类剪接变体hNKCC1A和hNKCC2A具有抑制作用[1]。布美他尼钠(0.03-100μM;5分钟)以剂量依赖性方式抑制表达NKCC1A的卵母细胞对86Rb+的摄取[1]。布美他尼钠抑制HEK-293细胞中NKCC2亚型B,IC50值为0.54μM[2]。
体内研究 布美他尼钠(7.6-30.4 mg/kg;静脉注射)可减弱皮层和纹状体表观扩散系数(ADC)比值的下降(40-67%),表明水肿形成减少[3]。布美他尼钠也可以减少梗死面积[3]。布美他尼钠在大鼠静脉注射2 mg/kg、8 mg/kg和20 mg/kg后分别显示出21.4分钟、53.8分钟和137分钟的不同半衰期[4]。
参考文献

[1]. Lykke K, et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 2016 Jun;59:42-9.

[2]. Ciaran Richardson, et al. Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways. J Cell Sci. 2011 Mar 1;124(Pt 5):789-800.

[3]. Martha E O'Donnell, et al. Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab. 2004 Sep;24(9):1046-56.

[4]. S H Lee, et al. Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1994 Feb;22(1):1-17.6

沸点 571.2ºC at 760mmHg
分子式 C17H19N2NaO5S
分子量 386.39800
闪点 299.3ºC
精确质量 386.09100
PSA 129.93000
LogP 3.55590
蒸汽压 6.89E-14mmHg at 25°C
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