盐酸维拉佐酮 T6232

Product Introduction
Bioactivity


英文名: Vilazodone Hydrochloride

描述: Vilazodone Hydrochloride (EMD 68843) 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。

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 9.6 mg/mL (20 mM)


关键字: Serotonin Receptor | SERT | 5-HT Receptor | Inhibitor | inhibit | Serotonin Transporter | Vilazodone Hydrochloride | Vilazodone | 5-HTT | 5-hydroxytryptamine Receptor | EMD-68843 | EMD68843 | SLC6A4

相关产品: MDL 100009 | (R)-Mirtazapine | Citalopram hydrobromide | Nefazodone hydrochloride | Volinanserin | Elemicin | PU02 | Rodatristat ethyl | PZ-1922 | Vabicaserin hydrochloride

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Anti-Cancer Approved Drug Library | Target-Focused Phenotypic Screening Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途