Trazodone effects on [3H]-paroxetine and α2-adrenoreceptors in platelets of patients with major depression
Donatella Marazziti, Giorgio Consoli, Francesca Golia, Stefano Baroni, Irene Masala, Marina Carlini, Mario Catena Dell’Osso
Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, University of Pisa, Pisa, Italy
Abstract: Trazodone is an antidepressant which behaves as a selective 5-HT2 antagonist and 5-HT reuptake inhibitor. The lack of information on its effects in vivo prompted us to evaluate α2-adrenoceptors by means of the specific binding of [3H]-rauwolscine, and the 5-HT transporter (SERT) by means of the binding of [3H]-paroxetine ([3H]-Par), in platelets of depressed patients, before and after one month of treatment with trazodone (75–300 mg/day). Twenty-five outpatients of both sexes with a diagnosis of major depression, as assessed by the Structured Clinical Interview for DSM IV, were included in the study. Depressive symptoms were evaluated by means of the Hamilton Rating Scale for Depression: the total score (mean ± SD) was 20 ± 6 at baseline (t0) and 7 ± 4 after one month of treatment (t1). Platelet membranes, [3H]-rauwolscine and [3H]-Par bindings were carried out according to standardized protocols. The results showed that the Bmax values of [3H]-Par were statistically lower at t1 than at t0 (733 ± 30 vs 1471 ± 99, P < 0.001), while the Kd and the [3H]-rauwolscine binding parameters remained unchanged. The findings of this study suggest that in vivo trazodone modifies the number of the SERT proteins and that, perhaps, most of its antidepressant properties are related to this activity.
Keywords: trazodone, depression, serotonin, platelets, α2-adrenoreceptors, [3H]-rauwolscine, serotonin transporter, [3H]-paroxetine
This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.Download Article [PDF]