Description
Vilazodone is a kind of serotonergic antidepressant developed by Merck KGaA Company. It is a novel compound with high affinity and selectivity for the 5-hydroxytrptamine (5-HT) transporter and 5-HT (1A) receptors. It is indicated for the treatment of major depressive disorder (MDD). It is can be used as an alternative drugs for other kind of antidepressant classes drugs that can’t be tolerated by patients. As a selective serotonin reuptake inhibitor, vilazodone can prevent the serotonin from re-entering into cell bodies, therefore making it remain longer inside the synapse. Moreover, it has a high selectivity for the serotonin-1A receptor, taking effect as a partial agonist that can simulate the production of serotonin. These effects result in increased serotonin in the synaptic cleft. This effect is related to the antidepressant effect of vilazodone in vivo.
References
https://www.drugbank.ca/drugs/DB06684
https://en.wikipedia.org/wiki/Vilazodone
http://www.rxlist.com/viibryd-drug/indications-dosage.htm
Description
In January 2011, the U.S. FDA approved vilazodone for the treatment of
major depressive disorder (MDD).
Vilazodone is a novel antidepressant agent that combines potent serotonin reuptake inhibition (IC
50=0.2 nM) with high affinity for 5-HT1A receptors (IC
50=0.5 nM)and partial 5-HT1A receptor agonist functional activity. Vilazodone has good
selectivity over other monoamine receptors and is efficacious in preclinical
models of depression in rats and mice. Vilazodone is an
indolylbutylpiperazine derivative that has been prepared by coupling of an
indolylbutyl chloride or tosylate with 5-(piperazin-1-yl)benzofuran-2-
carboxamide or the corresponding ester. The cyanoindole portion of
vilazodone is important for conferring high affinity for both the serotonin
transporter and the 5-HT1A receptor. Para-substitution on the phenyl
group attached to the piperidine moiety reduces affinity for dopamine
receptors, while the carboxamide group provides improved pharmacokinetic
properties.
Chemical Properties
Light Yellow Solid
Originator
Merck KGaA (Germany)
Uses
Labelled analogue of Vilazodone
Uses
It is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.
Uses
An inhibitor of ST and activator of SR-1A
Definition
ChEBI: A 1-benzofuran that is 5-(piperazin-1-yl}-1-benzofuran-2-carboxamide having a (5-cyanoindol-3-yl)butyl group attached at position N-4 on the piperazine ring. Used for the treatment of major depressive disorder.
