Ambroxol hydrochloride 是前药溴己辛的活性代谢产物，是一种葡糖脑苷脂酶伴侣，可增加葡糖脑苷脂酶的活性。它可刺激粘液纤毛作用并清除呼吸道中的空气通道，具有强效祛痰作用。它可诱导肺细胞自噬，有用于帕金森氏病和神经性戈谢病的研究潜力。

Ambroxol hydrochloride is a metabolite of BROMHEXINE that stimulates mucociliary action and clears the air passages in the respiratory tract. It is usually administered as the hydrochloride.

100 μM Ambroxol明显抑制嗜碱粒细胞中IgE抗体诱导的组胺,LTC4,IL-4 和IL-13的释放,降低单核细胞中由C5a或酵母聚糖诱导的组胺和LTB4释放.Ambroxol分别抑制由ConA和化合物48/80刺激的人类腺样体肥大细胞（1000 μM Ambroxol）和皮肤肥大细胞（100 μM Ambroxol）引起的组胺释放超过50％.Ambroxol还可以减少酵母聚糖或fMLP刺激的粒细胞中LTB4和超氧阴离子的产生.

Ambroxol在CNaIIA细胞中,表现得像带电荷的局部麻醉剂：阻断依赖于刺激次数,并随着一系列去极化刺激中频率的增加而增加。Ambroxol在CNaIIA细胞中,对失活通道抑制率比静息通道高5.5倍。Ambroxol对TTX-r和TTX-s通道中Na+电流动力学影响不同。TTX-r通道相应因子仅为3.3。Ambroxol抑制感觉神经元中Na+通道。对TTX-r 通道的强直性阻断效能较高。Ambroxol抑制人类白细胞和肥大细胞释放组胺,白三烯和细胞因子。

Standard HDAC Assays: Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. Km and Vmax values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme.

23828-92-4

C13H19Br2ClN2O

414.57

Mucosolvan;Ambroxol HCl;Mucoangin;盐酸氨溴索

DMSO:20.7 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years