2-(3-4-dimethoxyphenyl)-3-fluoroallylamine and tianeptine

Tianeptine is a substance enhancing the serotonir uptake while sertraline and clomipramine inhibit it. By means of 5-hydroxyin-doleacetic acid (5-HIAA) voltammetric measurements, this study investigated their influence on serotonin metabolism which depends mainly upon the activity of monoamine oxidase type A. After tianeptine injection the 5-HIAA signal increased by about 60%. This effect was maintained when the animals were pre-treated with MDL 72145 (an inhibitor of monoamine oxidase type B) but reduced when clorgyline (an inhibitor of monoamine oxidase type A) was administered after tianeptine. Administration of sertraline or clomipramine reduced the 5-HIAA signal by about 30-50%, whether the animals were pre-treated with MDL 72145 or not. It is to be concluded that tianeptine, sertraline and clomipramine can regulate the 5-HT fraction present in the synaptic cleft, not only by acting at the level of the serotoninergic neurons, but also by favoring or reducing the access of the amine to monoamine oxidase type A which is synthesized within non-serotoninergic neurons and glial cells.

Topics: 1-Naphthylamine; 3,4-Dihydroxyphenylacetic Acid; Allylamine; Animals; Antidepressive Agents; Brain; Clomipramine; Clorgyline; Electrochemistry; Hydroxyindoleacetic Acid; Male; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Rats; Rats, Inbred Strains; Selective Serotonin Reuptake Inhibitors; Serotonin; Sertraline; Thiazepines