1-(2-((2,4-DiMethylphenyl)thio)phenyl)piperazine;Vortioxetin;Trintellix (vortioxetine);Votigetin;Votexetine;Lu AA 21004;Vortioxetine;Vortioxetine,98%;1-(2-((2,4-DimethyL;Vortioxetine, >=99%
In September 2013, vortioxetine (also known as Lu AA21004) was approved in the United States for the treatment of major depressive disorder (MDD). Vortioxetine was discovered from a designed multiple ligand approach to identifying an antidepressant agent that combined SERT inhibition with 5-HT1A agonism to more rapidly desensitize 5-HT1A receptors and 5-HT3A antagonism to improve mood and cognitive function. Vortioxetine has a human SERT IC50=5.4 nM, an EC50=200 nM as a human 5-HT1A receptor agonist (efficacy=96%; Ki=39 nM), and an IC50=12 nM as a human 5-HT3A receptor antagonist (Ki=3.7 nM). It has weak inhibition of the dopamine and norepinephrine transporters, but high affinity for the human β1-noradrenergic receptor (Ki=46 nM), human 5-HT1B receptor (Ki=33 nM, partial agonist), and the human 5-HT-7 receptor (Ki=19 nM, antagonist).
History
Vortioxetine was invented by scientists at Lundbeck who reported the rationale and synthesis for the drug (then called Lu AA21004) in a 2011 paper. Takeda and Lundbeck Announce the U.S. Submission of a New Drug Application for Vortioxetine, an Investigational Drug for the Treatment of Major Depressive Disorder on Oct 1, 2012. Vortioxetine, which was approved by the Food and Drug Administration (FDA) on September 30, 2013, for treatment of major depressive disorder (MDD) , and Brintellix (vortioxetine) Renamed Trintellix (vortioxetine) in U.S. to Avoid Name Confusion.
Verwenden
Vortioxetine can be used in biological study of effectiveness of long term vortioxetine treatment of patients with major depressive disorder.
Definition
ChEBI: An N-arylpiperazine in which the aryl group is specified as 2-[(2,4-dimethylphenyl)sulfanyl]phenyl. Used (as its hydrobromide salt) for treatment of major depressive disorder.
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