product name Desvenlafaxine Succinate
Description: Desvenlafaxine Succinate (also known as WY 45233 Succinate) is a novel and potent serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively. Desvenlafaxine succinate is the succinate salt monohydrate of O-desmethylvenlafaxine, an active metabolite of venlafaxine.
References: J Pharmacol Exp Ther. 2006 Aug;318(2):657-65; Ann Pharmacother. 2008 Oct;42(10):1439-46.
381.46
Formula
C16H25NO2.C4H6O4.H2O
CAS No.
386750-22-7
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
other peoduct :
| 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
