Please use this identifier to cite or link to this item:
https://www.um.edu.mt/library/oar/handle/123456789/22594
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Di Giovanni, Giuseppe | - |
dc.contributor.author | Garcia, Isela | - |
dc.contributor.author | Colangeli, Roberto | - |
dc.contributor.author | Pierucci, Massimo | - |
dc.contributor.author | Rivadulla, Marcos L. | - |
dc.contributor.author | Soriano, Elena | - |
dc.contributor.author | Chioua, Mourand | - |
dc.contributor.author | Della Corte, Laura | - |
dc.contributor.author | Yanez, Matilde | - |
dc.contributor.author | De Deurwaerdère, Philippe | - |
dc.contributor.author | Fall, Yagamare | - |
dc.contributor.author | Marco-Contelles, Jose | - |
dc.date.accessioned | 2017-10-13T17:22:39Z | - |
dc.date.available | 2017-10-13T17:22:39Z | - |
dc.date.issued | 2014 | - |
dc.identifier.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. | en_GB |
dc.identifier.uri | https://www.um.edu.mt/library/oar//handle/123456789/22594 | - |
dc.description.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. | en_GB |
dc.language.iso | en | en_GB |
dc.publisher | Wiley-Blackwell Publishing Ltd. | en_GB |
dc.rights | info:eu-repo/semantics/restrictedAccess | en_GB |
dc.subject | Alzheimer's disease | en_GB |
dc.subject | Enzyme inhibitors | en_GB |
dc.subject | Monoamine oxidase | en_GB |
dc.subject | Temporal lobe epilepsy | en_GB |
dc.title | N-(furan-2-ylmethyl)-N-methylprop-2-yn-1-amine (F2MPA) : a potential cognitive enhancer with MAO inhibitor properties | en_GB |
dc.type | article | en_GB |
dc.rights.holder | The copyright of this work belongs to the author(s)/publisher. The rights of this work are as defined by the appropriate Copyright Legislation or as modified by any successive legislation. Users may access this work and can make use of the information contained in accordance with the Copyright Legislation provided that the author must be properly acknowledged. Further distribution or reproduction in any format is prohibited without the prior permission of the copyright holder. | en_GB |
dc.description.reviewed | peer-reviewed | en_GB |
dc.identifier.doi | 10.1111/cns.12284 | - |
dc.publication.title | CNS Neuroscience & Therapeutics | en_GB |
Appears in Collections: | Scholarly Works - FacM&SPB |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
F2MPA.pdf Restricted Access | 419.22 kB | Adobe PDF | View/Open Request a copy |
Items in OAR@UM are protected by copyright, with all rights reserved, unless otherwise indicated.