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Desvenlafaxine Succinate(WY 45233 O-Desmethylvenlafaxine)
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。
Desvenlafaxine Succinate(WY 45233 O-Desmethylvenlafaxine)图片
CAS NO:448904-47-0
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)381.46
FormulaC16H25NO2.C4H6O4.H2O
CAS No.386750-22-7 (Succinate hydrate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 80 mg/mL (209.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)0.5% methylcellulose+0.2% Tween 80: 30 mg/mL
SynonymsWY 45233 Succinate; WY-45233; Pristiq; WY45233; WY 45233; Desfax
实验参考方法
In Vitro

In vitro activity: 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. 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.

In VivoDesvenlafaxine 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. 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%.
Animal modelMale Sprague-Dawley rats
Formulation & DosageDissolved in 0.25% Tween 80 and 0.5% methylcellulose; 30 mg/kg; oral gavage
ReferencesJ Pharmacol Exp Ther. 2006 Aug;318(2):657-65; Ann Pharmacother. 2008 Oct;42(10):1439-46.