Desvenlafaxine Succinate(WY 45233 O-Desmethylvenlafaxine)

Molecular Weight (MW)	381.46
Formula	C16H25NO2.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
Synonyms	WY 45233 Succinate; WY-45233; Pristiq; WY45233; WY 45233; Desfax

Molecular Weight (MW)

381.46

Formula

C16H25NO2.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

Synonyms

WY 45233 Succinate; WY-45233; Pristiq; WY45233; WY 45233; Desfax

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 Vivo	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. 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 model	Male Sprague-Dawley rats
Formulation & Dosage	Dissolved in 0.25% Tween 80 and 0.5% methylcellulose; 30 mg/kg; oral gavage
References	J Pharmacol Exp Ther. 2006 Aug;318(2):657-65; Ann Pharmacother. 2008 Oct;42(10):1439-46.

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 Vivo

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. 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 model

Male Sprague-Dawley rats

Formulation & Dosage

Dissolved in 0.25% Tween 80 and 0.5% methylcellulose; 30 mg/kg; oral gavage

References

J Pharmacol Exp Ther. 2006 Aug;318(2):657-65; Ann Pharmacother. 2008 Oct;42(10):1439-46.

CAS NO:	448904-47-0
规格:	≥98%

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