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Neostigmine bromide

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Chemical Structure| 114-80-7 同义名 : 溴化新斯的明 ;Eustigmin bromide;Neoserine bromide
CAS号 : 114-80-7
货号 : A198984
分子式 : C12H19BrN2O2
纯度 : 98%
分子量 : 303.195
MDL号 : MFCD00011795
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(346.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(329.82 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 80 mg/mL clear

生物活性
靶点

  • AChR
描述 Neostigmine bromide is a reversible acetylcholine esterase inhibitor that binds to the anionic binding site of AChE. Administration of neostigmine, may successfully reverse some negative effects of inflammation on the GnRH (gonadotropin-releasing hormone) neurons[3]. As the molecular weight of neostigmine bromide is 303 g/mol and the steady-state volume of distribution is approximately 0.5 L/kg, its plasma concentration was calculated to be 0.13–0.46 μM. The dosage of neostigmine can be reduced properly when used to antagonize the residual neuromuscular block in septic patients[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03399890 - Completed - Turkey ... 展开 >> Ankara University Faculty of Medicine Ankara, Turkey 收起 <<
NCT03519633 Curarization, Postoperative Re... 展开 >>sidual 收起 << Phase 2 Not yet recruiting January 30, 2019 Italy ... 展开 >> Campus Bio-medico Recruiting Roma, RM, Italy, 00128 Contact: Corrado Terranova    06225411203 ext +39    c.terranova@unicampus.it 收起 <<
NCT03519724 Curarization, Postoperative Re... 展开 >>sidual 收起 << Phase 2 Not yet recruiting January 30, 2019 Italy ... 展开 >> Campus Bio-medico Recruiting Roma, RM, Italy, 00128 Contact: Corrado Terranova    06225411203 ext +39    c.terranova@unicampus.it 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.49mL

3.30mL

1.65mL

32.98mL

6.60mL

3.30mL
参考文献

[1]Khorshid AF, Issa YM. Modified carbon paste sensor for the potentiometric determination of neostigmine bromide in pharmaceutical formulations, human plasma and urine. Biosens Bioelectron. 2014 Jan 15;51:143-9.

[2]Trevisani GT, Hyman NH, et al. Neostigmine: safe and effective treatment for acute colonic pseudo-obstruction. Dis Colon Rectum. 2000 May;43(5):599-603.

[3]Herman AP, Tomaszewska-Zaremba D, Kowalewska M, Szczepkowska A, Oleszkiewicz M, Krawczyńska A, Wójcik M, Antushevich H, Skipor J. Neostigmine Attenuates Proinflammatory Cytokine Expression in Preoptic Area but Not Choroid Plexus during Lipopolysaccharide-Induced Systemic Inflammation. Mediators Inflamm. 2018 Oct 9;2018:9150207.

[4]Wu J, Jin T, Wang H, Li ST. Sepsis Strengthens Antagonistic Actions of Neostigmine on Rocuronium in a Rat Model of Cecal Ligation and Puncture. Chin Med J (Engl). 2016 Jun 20;129(12):1477-82.