product name Desvenlafaxine
Description: Desvenlafaxine (also known as WY 45233) 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 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.
References: J Pharmacol Exp Ther. 2006 Aug;318(2):657-65; Ann Pharmacother. 2008 Oct;42(10):1439-46.
263.38
Formula
C16H25NO2
CAS No.
93413-62-8
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
Synonyms
WY 45233
other peoduct :
| 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Desvenlafaxine 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 & 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. |
