Vortioxetine

Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM)[1][2].

[1]Bang-Andersen B, et al. Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011 May 12;54(9):3206-21.|[2]Guilloux JP, et al. Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice. Neuropharmacology. 2013 May 28;73C:147-159.|[3]Theunissen EL, et al. A randomized trial on the acute and steady-state effects of a new antidepressant, vortioxetine (Lu AA21004), on actual driving and cognition. Clin Pharmacol Ther. 2013 Jun;93(6):493-501.|[4]Rothschild AJ, et al. Vortioxetine (Lu AA21004) 5mg in generalized anxiety disorder: results of an 8-week randomized, double-blind, placebo-controlled clinical trial in the United States. Eur Neuropsychopharmacol. 2012 Dec;22(12):858-66.|[5]Mrk A, et al. Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J Pharmacol Exp Ther. 2012 Mar;340(3):666-75.Antioxidants (Basel). 2024 May 29;13(6):667.|Biomedicines. 2022 Jun 3;10(6):1318.|bioRxiv. 2024 Feb 9:2024.02.08.579543.|Eur Arch Psychiatry Clin Neurosci. 2023 Mar;77(3):149-159.|Nature. 2023 Dec;624(7992):672-681.|Neurobiol Dis. 2024 Oct 1:200:106651.|Psychiat Res. November 2022, 114838.|Psychiatry Res. 2022 Nov;317:114838.|Mol Pharmacol. 2023 Nov;104(5):230-238.