ビラゾドン 化学特性,用途語,生産方法
効能
抗うつ薬, セロトニン受容体拮抗・再取り込み阻害薬
説明
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.
化学的特性
Light Yellow Solid
使用
Labelled analogue of Vilazodone
定義
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.
ビラゾドン 上流と下流の製品情報
原材料
準備製品