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Title

N-(furan-2-ylmethyl)-N-methylprop-2-yn-1-amine (F2MPA): A potential cognitive enhancer with MAO inhibitor properties

AuthorsDi Giovanni, Giuseppe; García, Isela; Colangeli, Roberto; Pierucci, Massimo; Rivadulla, Marcos L.; Soriano, Elena ; Chioua, Mourad ; Della Corte, Laura; Yáñez, Matilde; De Deurwaerdère, Phillippe; Fall, Yagamare; Marco-Contelles, José
KeywordsADMET
Alzheimer's disease
Enzyme inhibition
Kinetics
Long-term potentiation
MAO-A
MAO-B
Temporal lobe epilepsy
Issue Date2014
PublisherJohn Wiley & Sons
CitationCNS Neuroscience and Therapeutics 20: 633- 640 (2014)
AbstractBackground: 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. © 2014 John Wiley & Sons Ltd.
URIhttp://hdl.handle.net/10261/101161
DOI10.1111/cns.12284
Identifiersdoi: 10.1111/cns.12284
issn: 1755-5930
e-issn: 1755-5949
Appears in Collections:(IQOG) Artículos
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