Galanthamine

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Chemical Structure| 357-70-0 同义名 : Galantamine; NSC 100058; Lycoremine; Reminyl; Razadyne ER; Razadyne; Nivalin
CAS号 : 357-70-0
货号 : A697166
分子式 : C17H21NO3
纯度 : 98%
分子量 : 287.35
MDL号 : MFCD00867189
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Galanthamine is selective for acetylcholinesterase versus butyrylcholinesterase. Galanthamine attenuates drug-and lesion-induced cognitive deficits in animal models of learning and memory[1]. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs (accessory subunits in heteromeric nicotinic receptors) expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes[2]. Acute administration of galantamine (0.3-3 mg/kg, i.p.) increased IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) caused a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it did not affect the mRNA levels of other neurotrophic/growth factors[3]. Galantamine treatment prevented LPS-induced (lipopolysaccharide) deficits in spatial learning and memory as well as memory acquisition of the passive avoidance response. Galantamine reduced the inflammatory response not only in the BV-2 microglia cell line, but also in the HT-22 hippocampal neuronal cell line[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.80mL

6.96mL

3.48mL

参考文献

[1]Fulton B, Benfield P. Galanthamine. Drugs Aging. 1996 Jul;9(1):60-5; discussion 66-7

[2]Kuryatov A, Onksen J, Lindstrom J. Roles of accessory subunits in alpha4beta2(*) nicotinic receptors. Mol Pharmacol. 2008 Jul;74(1):132-43

[3]Kita Y, Ago Y, Takano E, Fukada A, Takuma K, Matsuda T. Galantamine increases hippocampal insulin-like growth factor 2 expression via α7 nicotinic acetylcholine receptors in mice. Psychopharmacology (Berl). 2013 Feb;225(3):543-51

[4]Liu Y, Zhang Y, Zheng X, Fang T, Yang X, Luo X, Guo A, Newell KA, Huang XF, Yu Y. Galantamine improves cognition, hippocampal inflammation, and synaptic plasticity impairments induced by lipopolysaccharide in mice. J Neuroinflammation. 2018 Apr 18;15(1):112