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