5-HTT and 5-HT1A receptor occupancy of the novel substance vortioxetine (Lu AA21004). A PET study in control subjects

@article{Stenkrona20135HTTA5,
  title={5-HTT and 5-HT1A receptor occupancy of the novel substance vortioxetine (Lu AA21004). A PET study in control subjects},
  author={Per Stenkrona and Christer Halldin and Johan Lundberg},
  journal={European Neuropsychopharmacology},
  year={2013},
  volume={23},
  pages={1190-1198}
}

Effect of clinically relevant doses of vortioxetine and citalopram on serotonergic PET markers in the nonhuman primate brain

Comparing its effect to the SSRI citalopram on the binding of [11C]AZ10419369 to the 5-HT1B receptor in the nonhuman primate brain suggests that vortioxetine binds to the5-HT 1B receptor at clinically relevant doses.

Effects of acute and sustained administration of vortioxetine on the serotonin system in the hippocampus: electrophysiological studies in the rat brain

Results indicate that this compound acted as a 5-HT1B receptor partial agonist and decreased the function of terminal 5- HT1B autoreceptor following its sustained administration, which may contribute to the antidepressant effect of vortioxetine.

Vortioxetine: First Global Approval

Animal and in vitro studies indicate that several neurotransmitter systems may be impacted by vortioxetine, with the drug enhancing levels of 5-HT, noradrenaline, dopamine, acetylcholine and histamine in certain areas of the brain, as well as modulating γ-aminobutyric acid and glutamate neurotransmission.

PET studies on the mechanisms of action of antidepressant and antipsychotic drugs

The results suggest that vortioxetine binds to the 5-HT1B receptor when administered at clinically relevant doses, and can be translated into future human studies.

The efficacy of vortioxetine for the treatment of major depressive disorder

This review attempts to compile the efficacy profile of vortioxetine in different clinical trials and the results are compared with other standard antidepressants.

Vortioxetine: a novel antidepressant for the treatment of major depressive disorder

Vortioxetine’s unique psychopharmacological properties might contribute to an improved clinical outcome in MDD patient populations as described in published preclinical and clinical studies and product labels.

Integrated Strategy for Use of Positron Emission Tomography in Nonhuman Primates to Confirm Multitarget Occupancy of Novel Psychotropic Drugs: An Example with AZD3676

The properties of AZD3676 showed preclinical properties consistent with CNS drug potential, including nanomolar receptor affinity and efficacy in rodent models of learning and memory, and these findings support the further integrated use of PET for confirmation of multitarget occupancy of CNS drugs.

Vortioxetine: Clinical Pharmacokinetics and Drug Interactions

Vortioxetine is a novel antidepressant with multimodal activity currently approved for the treatment of major depressive disorder. Vortioxetine is orally administered once daily at 5- to 20-mg doses.
...

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