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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|
Rivadulla, Marcos L.
Della Corte, Laura
De Deurwaerdere, Philippe
Temporal lobe epilepsy
|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.|
|Appears in Collections:||Scholarly Works - FacM&SPB|
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