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Vilazodone Hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vilazodone Hydrochloride图片
CAS NO:163521-08-2
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
EMD 68843
盐酸维拉佐酮
SB659746A
Vilazodone HCl
产品介绍
Vilazodone Hydrochloride 是 5-HT1A 受体和特异性 5-羟色胺再摄取抑制剂 (SSRI) 的部分激动剂,用于治疗重度抑郁症。

产品描述

Vilazodone HCl, a partial agonist of 5-HT1A receptors and specific serotonin reuptake inhibitor (SSRI), is utilized in treating of the major depressive disorder.

体外活性

Vilazodone demonstrates an IC50 of 0.2 nM at the human 5-HT1A receptor and 0.5 nM for the SERT. Vilazodone displays high affinity (pKi ≥ 9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A receptors. [1]

体内活性

Vilazodone selectively enhances serotonergic output in the prefrontal cortex of rats. Vilazodone demonstrates anxiolytic efficacy through Behavioral evaluations in the ultrasonic vocalization model of anxiety in rats. Vilazodone also shows efficacy but at a single dose only in the forced swim test (a putative model of depression). [1] Vilazodone (1-10 mg/kg p.o.) dose-dependently displaces in vivo [3H]DASB (N,N-dimethyl-2-(2-amino-4-cyanophenylthio)benzylamine) binding from rat cortex and hippocampus, indicating that vilazodone occupies 5-HT transporters in vivo. Vilazodone (10 mg/kg p.o.) is demonstrated to cause a 2-fold increase in extracellular 5-HT but no change in noradrenaline or dopamine levels in frontal cortex of freely moving rats. [2] Vilazodone affects stress potentiation of startle at doses above 5 mg/kg in rats. Vilazodone increases stress elevation of startle at 10 mg/kg in rats. Vilazodone (20 and 40 mg/kg) blocked stress potentiation of startle in rats. Vilazodone increases stress elevation of startle at all doses in rats. [3] vilazodone has no effect on 5-HT efflux at 100 nM but significantly decreases 5-HT efflux at 1 mM in the guinea-pig dorsal raphe nucleus. Vilazodone significantly increases the re-uptake half life for 5-HT in the guinea-pig dorsal raphe nucleus. [4]

Cas No.

163521-08-2

分子式

C26H28ClN5O2

分子量

477.99

别名

EMD 68843;盐酸维拉佐酮;SB659746A;Vilazodone HCl

储存和溶解度

DMSO:9.6 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years