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Desvenlafaxine(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(WY 45233 O-Desmethylvenlafaxine)图片
CAS NO:93413-62-8
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)263.38
FormulaC16H25NO2
CAS No.93413-62-8 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 37 mg/mL (140.5 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (11.4 mM)
Solubility (In vivo)0.5% methylcellulose+0.2% Tween 80: 30 mg/mL
SynonymsWY-45233; WY45233; WY 45233; Pristiq; Desfax
实验参考方法
In Vitro

In vitro activity: Desvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, desvenlafaxine inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine 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, which could impact the metabolism of drugs metabolized via this enzyme.

In VivoDesvenlafaxine rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. Desvenlafaxine 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 model Male 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.