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Title: N-(furan-2-ylmethyl)-N-methylprop-2-yn-1-amine (F2MPA) : a potential cognitive enhancer with MAO inhibitor properties
Authors: Di Giovanni, Giuseppe
Garcia, Isela
Colangeli, Roberto
Pierucci, Massimo
Rivadulla, Marcos L.
Soriano, Elena
Chioua, Mourand
Della Corte, Laura
Yanez, Matilde
De Deurwaerdere, Philippe
Fall, Yagamare
Marco-Contelles, Jose
Keywords: Alzheimer's disease
Enzyme inhibitors
Monoamine oxidase
Temporal lobe epilepsy
Issue Date: 2014
Publisher: Wiley-Blackwell Publishing Ltd.
Citation: Di Giovanni, G., García, I., Colangeli, R., Pierucci, M., Rivadulla, M. L., Soriano, E...,Marco-Contelles, J. (2014). N-(furan-2-ylmethyl)-N-methylprop-2-yn-1-amine (F2MPA) : a potential cognitive enhancer with MAO inhibitor properties. CNS Neuroscience & Therapeutics, 20(7), 633-640.
Abstract: Background: A considerable body of human and animal experimental evidence links monoaminergic systems and cognition. Monoamine oxidase inhibitors (MAOIs), 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 (F2MPA), 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, F2MPA improves DG synaptic transmission without triggering pathological hyperexcitability. Therefore, F2MPA shows promise as a potential cognition-enhancing therapeutic drug.
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