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• W2022732091 abstract "Various types of anticholinesterasic agents have been used to improve the daily activities of Alzheimer's disease patients. It was recently demonstrated that Galantamine, described as a molecule with anticholinesterasic properties, is also an allosteric enhancer of human α 4 β 2 neuronal nicotinic receptor activity. We explored its effect on the human α 7 neuronal nicotinic acetylcholine receptor (nAChR) expressed in Xenopus oocytes. Galantamine, at a concentration of 0.1 μ M , increased the amplitude of acetylcholine (ACh)‐induced ion currents in the human α 7 nAChR expressed in Xenopus oocytes, but caused inhibition at higher concentrations. The maximum effect of galantamine, an increase of 22% in the amplitude of ACh‐induced currents, was observed at a concentration of 250 μ M Ach. The same enhancing effect was obtained in oocytes transplanted with Torpedo nicotinic acetylcholine receptor (AChR) isolated from the electric organ, but in this case the optimal concentration of galantamine was 1 μ M . In this case, the maximum effect of galantamine, an increase of 35% in the amplitude of ACh‐induced currents, occurred at a concentration of 50 μ M ACh. Galantamine affects not only the activity of post‐synaptic receptors but also the activity of nerve terminals. At a concentration of 1 μ M , quantal spontaneous events, recorded in a cholinergic synapse, increased their amplitude, an effect which was independent of the anticholinesterasic activity associated with this compound. The anticholinesterasic effect was recorded in preparations treated with a galantamine concentration of 10 μ M . In conclusion, our results show that galantamine enhances human α 7 neuronal nicotinic ACh receptor activity. It also enhances muscular AChRs and the size of spontaneous cholinergic synaptic events. However, only a very narrow range of galantamine concentrations can be used for enhancing effects. British Journal of Pharmacology (2005) 145 , 672–678. doi: 10.1038/sj.bjp.0706221" @default.
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• W2022732091 date "2005-07-01" @default.
• W2022732091 modified "2023-10-18" @default.
• W2022732091 title "Effect of galantamine on the human <i>α</i> 7 neuronal nicotinic acetylcholine receptor, the <i>Torpedo</i> nicotinic acetylcholine receptor and spontaneous cholinergic synaptic activity" @default.
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• W2022732091 doi "https://doi.org/10.1038/sj.bjp.0706221" @default.
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