163521-12-8 Usage
Description
Vilazodone, developed by Merck KGaA Company, is a serotonergic antidepressant 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) and can be used as an alternative for patients who cannot tolerate other antidepressant classes. Vilazodone functions as a selective serotonin reuptake inhibitor, preventing serotonin from re-entering cell bodies and prolonging its presence in the synapse. Additionally, it acts as a partial agonist for the serotonin-1A receptor, stimulating serotonin production and increasing its levels in the synaptic cleft, which contributes to its antidepressant effect in vivo. Vilazodone is a light yellow solid and is marketed under the brand name Viibryd.
Uses
Used in Pharmaceutical Industry:
VILAZODONE is used as an antidepressant for the treatment of major depressive disorder (MDD). It is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist, providing an alternative for patients who cannot tolerate other antidepressant classes.
Used in Clinical Evaluation:
VILAZODONE is used as a labeled analogue for clinical evaluation in the treatment of major depression, offering a novel compound with potent serotonin reuptake inhibition and high affinity for 5-HT1A receptors.
Used in Antidepressant Research:
VILAZODONE is used as an inhibitor of serotonin reuptake and activator of 5-HT1A receptors in preclinical models of depression in rats and mice, demonstrating efficacy and good selectivity over other monoamine receptors.
Approved by U.S. FDA:
In January 2011, the U.S. FDA approved VILAZODONE for the treatment of major depressive disorder (MDD), recognizing its potential as a novel antidepressant agent with unique properties and benefits for patients.
References
https://www.drugbank.ca/drugs/DB06684
https://en.wikipedia.org/wiki/Vilazodone
http://www.rxlist.com/viibryd-drug/indications-dosage.htm
Originator
Merck KGaA (Germany)
Check Digit Verification of cas no
The CAS Registry Mumber 163521-12-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,6,3,5,2 and 1 respectively; the second part has 2 digits, 1 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 163521-12:
(8*1)+(7*6)+(6*3)+(5*5)+(4*2)+(3*1)+(2*1)+(1*2)=108
108 % 10 = 8
So 163521-12-8 is a valid CAS Registry Number.
163521-12-8Relevant articles and documents
Preparation method of vilazodone
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Paragraph 0033-0052, (2021/02/06)
The invention relates to a preparation method of vilazodone. The preparation method comprises the steps of by using a compound 1 and a compound 2 as raw materials, carrying out one-step reaction underthe condition that trifluoroacetic acid is used as a solvent to obtain a compound I, namely the vilazodone. Compared with the prior art, the method has the advantages of short reaction route, easy post-treatment, high yield, cheap and easily available reagents used in the reaction, convenient operation, simple post-treatment, low cost, small environmental pollution, and suitableness for industrial production of vilazodone.
Preparation method of vilazodone hydrochloride
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Page/Page column 8-11, (2019/02/04)
The invention discloses a preparation method of vilazodone hydrochloride. The preparation method comprises the following steps: (1) in the presence of ammonium hydroxide or ammonium hydroxide and N-methylpyrrolidone, enabling 5-(1-piperazinyl)-benzofuran-2-ethyl formate hydrochloride to be subjected to ammonolysis reaction to obtain 5-(1-piperazinyl)-benzofuran-2-formamide; (2) in the presence ofalkali, enabling the 5-(1-piperazinyl)-benzofuran-2-formamide and 3-(4-chlorobutyl) indole-5-formonitrile to be subjected to nucleophilic substitution reaction to obtain a crude product of vilazodone,wherein the alkali is mixed alkali of sodium iodide, N,N-diisopropylethylamine and triethylamine or 1,8-diazabicycloundec-7-ene; (3) refining the crude product of vilazodone to obtain a refined product of vilazodone; and (4) enabling the refined product of vilazodone to be subjected to salt-forming reaction to obtain the vilazodone hydrochloride. By virtue of the ammonolysis reaction and the nucleophilic substitution reaction, the yield is higher, and the purity is higher; and the yield of the vilazodone hydrochloride is increased.
PROCESS FOR PREPARATION OF VILAZODONE, NOVEL INTERMEDIATES THEREOF AND NOVEL CRYSTALLINE FORM THEREOF
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, (2016/11/17)
The invention relates to process for preparation of Vilazodone and novel intermediates for synthesis of Vilazodone. The invention also relates to novel crystalline form of Vilazodone hydrochloride and process for preparation thereof.