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Galanthamine HBr

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Chemical Structure| 1953-04-4 同义名 : Galantamine hydrobromide;Galanthamine hydrobromide;NSC 100058;Galanthamine;Galantamine (hydrobromide)
CAS号 : 1953-04-4
货号 : A523680
分子式 : C17H22BrNO3
纯度 : 98%
分子量 : 368.27
MDL号 : MFCD00067672
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(32.59 mM)，配合低频超声，并水浴加热至45℃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: 15 mg/mL(40.73 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • AChE

    AChE, IC50:0.35 μM
描述 Galanthamine Hydrobromide is acetylcholinesterase inhibitor (AChEI) and a neuroactive drug capable of passing through the blood–brain barrier and can slow down the effects of AD[3]. Incubation of the cells for 48 h with 300 nM galantamine doubled the density of α7 nicotinic receptors and tripled the expression of the antiapoptotic protein Bcl-2[4]. Moreover, pretreatment with galantamine (8 mg/kg, i.m.) prevented the reduction of EPSC (excitatory postsynaptic currents) frequency observed at 6-9 days after the soman challenge[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.58mL

2.72mL

1.36mL

27.15mL

5.43mL

2.72mL
参考文献

[1]Pereira EF, Alkondon M, et al. Physostigmine and galanthamine: probes for a novel binding site on the alpha 4 beta 2 subtype of neuronal nicotinic acetylcholine receptors stably expressed in fibroblast cells. J Pharmacol Exp Ther. 1994 Aug;270(2):768-78.

[2]Thomsen T, Kaden B, et al. Inhibition of acetylcholinesterase activity in human brain tissue and erythrocytes by galanthamine, physostigmine and tacrine. Eur J Clin Chem Clin Biochem. 1991 Aug;29(8):487-92.

[3]Woo FY, Basri M, Masoumi HR, Ahmad MB, Ismail M. Formulation optimization of galantamine hydrobromide loaded gel drug reservoirs in transdermal patch for Alzheimer's disease. Int J Nanomedicine. 2015 Jun 5;10:3879-86.

[4]Arias E, Alés E, Gabilan NH, Cano-Abad MF, Villarroya M, García AG, López MG. Galantamine prevents apoptosis induced by beta-amyloid and thapsigargin: involvement of nicotinic acetylcholine receptors. Neuropharmacology. 2004 Jan;46(1):103-14.

[5]Alexandrova EA, Alkondon M, Aracava Y, Pereira EF, Albuquerque EX. Galantamine prevents long-lasting suppression of excitatory synaptic transmission in CA1 pyramidal neurons of soman-challenged guinea pigs. Neurotoxicology. 2014 Sep;44:270-8.