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Comparative Analysis of the Neurochemical Profile and MAO Inhibition Properties of N-(Furan-2-ylmethyl)-N-methylprop-2-yn-1-amine

AutorDe Deurwaerdère, Phillippe; Binda, Claudia; Corne, R.; Leone, C.; Valeri, A.; Valoti, M.; Ramsay, R. R.; Fall, Y.; Marco-Contelles, José
Palabras claveEnzymology
Alzheimer’s disease
Neuroprotection
Monoamine neurochemistry
Crystallography
Propargylamines
Fecha de publicación2017
EditorAmerican Chemical Society
CitaciónACS Chemical Neuroscience 8: 1026-1035 (2017)
ResumenThe regulation of brain monoamine levels is paramount for cognitive functions, and the monoamine oxidase (MAO A and B) enzymes play a central role in these processes. The aim of this study was to evaluate whether the procognitive properties exerted by propargylamine N-(furan-2-ylmethyl)-N-methylprop-2-yn-1-amine (F2MPA) are related to changes in monoamine content via MAO inhibition. In vivo microdialysis and ex vivo amine metabolite measurement demonstrated region-specific alterations in monoamine metabolism that differ from both of the classic MAO A and MAO B inhibitors, clorgyline and l-deprenyl, respectively. Although all the inhibitors (1 and 4 mg/kg) increased cortical serotonin tissue content, only F2MPA increased the levels of cortical noradrenaline. In the striatum, clorgyline (1 mg/kg), but not F2MPA (1 mg/kg), reduced extracellular levels of dopamine metabolites at rest or stimulated by the intrastriatal application of the MAO substrate 3-methoxytyramine. In vitro, F2MPA exhibited a low affinity toward MAO B and MAO A. Nonetheless, it modified the B form of MAO, forming a flavin adduct structurally similar to that with deprenyl. F2MPA was rapidly metabolized in the presence of rat but not human microsomes, producing a hydroxylated derivative. In conclusion, the effect of F2MPA on cognition may arise from monoaminergic changes in the cortex, but the role of MAO in this process is likely to be negligible, consistent with the poor affinity of F2MPA for MAO.
Versión del editorhttp://dx.doi.org/10.1021/acschemneuro.6b00377
URIhttp://hdl.handle.net/10261/154964
DOI10.1021/acschemneuro.6b00377
Identificadoresdoi: 10.1021/acschemneuro.6b00377
issn: 1948-7193
e-issn: 1948-7193
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