FA-70, a novel selective and irreversible monoamine oxidase-A inhibitor: effect on monoamine metabolism in mouse cerebral cortex
by
Moron JA, Perez V, Pasto M, Lizcano JM, Unzeta M
Departament Bioquimica i Biologia Molecular,
Facultat de Medicina,
Universitat Autonoma de Barcelona,
Campus Universitari de Bellaterra,
Barcelona, Spain.
J Pharmacol Exp Ther 2000 Feb; 292(2):788-94


ABSTRACT

A series of indolealkylamine derivatives has been previously designed and evaluated with the aim of finding the most potent and selective novel monoamine oxidase (MAO) inhibitors to be used in the therapy of neurological and affective disorders. Among them, FA70, a 5-hydroxy-indolealkylamine derivative, has been characterized in vitro as a potent, irreversible, and mechanism-based inhibitor of the MAO-A isoform. The comparison with clorgyline, analyzed under the same experimental conditions, confirmed FA70 as the most potent MAO-A inhibitor. The ex vivo effect of FA70 on MAO activity in mouse cerebral cortex was similar to that observed in vitro, showing more efficacy than in peripheral tissues. The ex vivo effect of FA70 on amine metabolism also was evaluated after acute and chronic treatment, and the results showed that between both MAO isoforms, MAO-A is the only one responsible for monoamine metabolism in this region of the brain. The ex vivo effect of FA70 on dopamine content was correlated with the activation effect on tyrosine hydroxylase activity, the enzyme responsible for the regulation of the limiting step in catecholamine synthesis.
MAO
RIMAs
MAOIs
Reward
Phenelzine
Safinamide
Befloxatone
Brofaromine
Moclobemide
Isocarboxazid
The MAOI Diet
Tranylcypromine
MAO interactions


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