Serotonin transporter occupancy with TCAs and SSRIs: a PET study in patients with major depressive disorder.

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Lundberg J, Tiger M, Landen M, Halldin C, Farde L

Serotonin transporter occupancy with TCAs and SSRIs: a PET study in patients with major depressive disorder.

Int J Neuropsychopharmacol. 2012 Sep;15(8):1167-72. doi: 10.1017/S1461145711001945. Epub 2012 Jan 16.

PubMed ID

22243688 [ View in PubMed

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Abstract

The aim of the present clinical positron emission tomography study was to examine if the 5-HTT is a common target, both for tricyclic antidepressants (TCAs) and selective serotonin reuptake inhibitors (SSRIs). Serotonin transporter (5-HTT) occupancy was estimated during treatment with TCA, SSRI and mirtazapine in 20 patients in remission from depression. The patients were recruited from out-patient units and deemed as responders to antidepressive treatment. The radioligand [(1)(1)C]MADAM was used to determine the 5-HTT binding potential. The mean 5-HTT occupancy was 67% (range 28-86%). There was no significant difference in 5-HTT occupancy between TCA (n=5) and SSRI (n=14). 5-HTT affinity correlated with the recommended clinical dose. Mirtazapine did not occupy the serotonin transporter. The results support that TCAs and SSRIs have a shared mechanism of action by inhibition of 5-HTT.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Mirtazapine	Sodium-dependent serotonin transporter	Protein	Humans	Unknown	Substrate Inhibitor	Details