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- W2171595778 abstract "Summary Background A considerable body of human and animal experimental evidence links monoaminergic systems and cognition. Monoamine oxidase inhibitors ( MAOI s), being able to enhance monoaminergic transmission and having neuroprotective properties, might represent a promising therapeutic strategy in cognitive impairment in Alzheimer's disease ( AD ) and other dementias. Methods The MAO ‐A and MAO ‐B inhibition profile of N‐(furan‐2‐ylmethyl)‐N‐prop‐2‐yn‐1‐amine derivates (compounds 1–3) were evaluated by fluorimetric method and their absorption, distribution, metabolism, excretion, and toxicity ( ADMET ) properties estimated. The effects of the selected compound 1, N‐(furan‐2‐ylmethyl)‐N‐methylprop‐2‐yn‐1‐amine (F2 MPA ), were evaluated on the basic synaptic transmission, long‐term potentiation ( LTP ), and excitability in the dentate gyrus (DG) of the hippocampus of anesthetized rats. Results F2MPA is a partially reversible inhibitor of hMAO ‐B, with moderate to good ADMET properties and drug‐likeness. Intraperitoneal administration of 1 mg/kg F2MPA greatly enhanced basic synaptic transmission, induced LTP, and potentiated electrically induced LTP in the dentate gyrus. Moreover, F2MPA did not modify seizure threshold of pilocarpine‐induced convulsion in CD1 mice. Conclusion Our findings suggest that, the MAO ‐B inhibitor, F2 MPA improves DG synaptic transmission without triggering pathological hyperexcitability. Therefore, F2 MPA shows promise as a potential cognition‐enhancing therapeutic drug." @default.
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- W2171595778 date "2014-05-21" @default.
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- W2171595778 title "<i>N</i>-(furan-2-ylmethyl)-<i>N</i>-methylprop-2-yn-1-amine (F2MPA): A Potential Cognitive Enhancer with MAO Inhibitor Properties" @default.
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- W2171595778 doi "https://doi.org/10.1111/cns.12284" @default.
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