盐酸沃替西汀 T2395L

Product Introduction
Bioactivity


英文名: Vortioxetine hydrobromide

描述: Vortioxetine hydrobromide (Lu AA21004 hydrobromide) 是5-HT1A、5-HT1B、5-HT3A、5-HT7受体和5-羟色胺转运体(SERT)的抑制剂，Ki 值分别为 15、33、3.7、19 和 1.6 nM。

激酶实验: Assay of MEK Kinase Activity: Anti-MEK1 antibody is used to immunoprecipitate MEK1 molecules. MEK kinase activity is measured as the ability of immuno-isolated MEK1 to activate recombinant ERK1 in a coupled assay using MBP as the end point of the assay. Phosphorylated MBP is resolved on a 14% SDS-PAGE gel and vacuum-dried before exposure to X-ray film.

体外活性: 皮下注射Lu AA21004（2.5-10.0 mg/kg）到大鼠的内侧前额叶皮层和腹侧海马区,可使细胞外5-HT,DA和NA的水平提高.皮下注射Lu AA21004（5 mg/kg）到大鼠的腹侧海马区,可提高细胞外5-HT水平 (200%).注射Lu AA21004（5 和10 mg/kg）20分钟后,ACh的水平得到提高,分别提高至224%和204%.Lu-AA21004（5 和10 mg/kg）到清醒大鼠腹侧的海马区,增强细胞外5-HT的水平.Lu-AA21004（5 和10 mg/kg）处理内侧前额叶皮层3天后,使5-HT的基础水平明显提高.Lu AA21004（10 mg/kg）可使大鼠的痛觉明显降低.在大鼠体内,Lu-AA21004的肝脏清除力及口服生物有效性分别为7.1(L/h)/kg和16%.Lu AA21004剂量依赖性影响大鼠的Bezold-Jarisch反射,抑制短暂的心动过缓（ED50：0.11 mg/kg）.

体内活性: Lu AA21004是h5-HT1B受体激动剂（EC50：460 nM）,全细胞检测中内在活性为22%。Lu-AA21004抑制重组人类CYP1A2（IC50：40 μM）,CYP2C9（IC50：39 μM）, CYP2D6（IC50：9.8 μM）和CYP3A4（IC50：10 μM）。在体外全细胞cAMP检测中,Lu AA21004结合到r5-HT7受体上（Ki：200 nM）。Lu AA21004是r5-HT7受体的一种功能性拮抗剂（IC50：2 μM）。

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

溶解度: Ethanol : 14 mg/mL (36.9 mM)
DMSO : 45 mg/mL (118.62 mM)


关键字: Lu AA21004 | 5-HTT | Lu AA 21004 | Serotonin Receptor | Inhibitor | Serotonin Transporter | SLC6A4 | Lu AA-21004 Hydrobromide | Vortioxetine hydrobromide | Lu AA21004 Hydrobromide | 5-HT Receptor | SERT | Vortioxetine | Vortioxetine Hydrobromide | Lu AA 21004 Hydrobromide | Lu AA-21004 | inhibit | 5-hydroxytryptamine Receptor

相关产品: 5-HT1A modulator 2 hydrochloride | Ro60-0175 | pCPA methyl ester hydrochloride | YM348 | Itasetron | Tegaserod maleate | Idalopirdine Hydrochloride | 5-HT2A&5-HT2C agonist-1 | Isobutyryl-L-carnitine | Deramciclane

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Serotonin Receptor-Targeted Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug 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