琥珀酸去甲文拉法辛 T6188

Product Introduction
Bioactivity


英文名: Desvenlafaxine succinate hydrate

描述: Desvenlafaxine succinate hydrate (WY 45233 Succinate) 是 Venlafaxine 主要代谢物的丁二酸盐形式，在人多巴胺转运体上显示弱的结合亲和力。它是具有口服活性的、能透过血脑屏障的5-HT 和 去甲肾上腺素再摄取的抑制剂，对 hSERT 和 hNET 的IC50值分别为47.3 nM 和531.3 nM。

体外活性: Desvenlafaxine succinate is the succinate salt monohydrate of O-desmethylvenlafaxine, an active metabolite of venlafaxine. Desvenlafaxine Succinate is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, Desvenlafaxine Succinate inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine Succinate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine Succinate inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively.[1] Desvenlafaxine Succinate has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with Desvenlafaxine Succinate, which could impact the metabolism of drugs metabolized via this enzyme. [2]

体内活性: Desvenlafaxine Succinate rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine Succinate significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. [1] Desvenlafaxine Succinate exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5%.[2]

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

溶解度: DMSO : 50 mg/mL (125.16 mM)


关键字: Desvenlafaxine succinate Hydrate | Inhibitor | O-Desmethylvenlafaxine succinate Hydrate | inhibit | Desvenlafaxine succinate hydrate | Serotonin Transporter | WY45233 Succinate | O-Desmethylvenlafaxine succinate | SERT | 5-HTT | WY-45233 Succinate | SLC6A4

相关产品: Brilaroxazine | Agomelatine | 8-OH-Dpat | Cinchonidine | Ramosetron hydrochloride | Ansofaxine hydrochloride | Asenapine Maleate | Capeserod | Arotinolol hydrochloride | RU 24969

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Parkinson's Disease Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Antidepressant Compound Library | Inhibitor Library | GPCR Compound Library | Serotonin Receptor-Targeted Compound Library | Anti-Cancer Approved Drug Library

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