[CAS NO. 93413-62-8]  Desvenlafaxine

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PRODUCTS SPECIFICATIONS [93413-62-8]

Store
Catalog
SLK-S4113
Brand
Selleck
CAS
93413-62-8

DESCRIPTION [93413-62-8]

Overview

MDLMFCD00871934
Molecular Weight263.38
Molecular FormulaC16H25NO2
SMILESC(CN(C)C)(C1(O)CCCCC1)C2=CC=C(O)C=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM3.7968 mL18.9840 mL37.9680 mL
5 mM0.7594 mL3.7968 mL7.5936 mL
10 mM0.3797 mL1.8984 mL3.7968 mL
50 mM0.0759 mL0.3797 mL0.7594 mL

Description

Desvenlafaxine (WY 45233 Succinate) is a and reuptake inhibitor with of 40.2 nM and 558.4 nM, respectively.

Features

Desvenlafaxine is a major active metabolite of venlafaxine.

Targets

5-HT [1]Norepinephrine (NE) [1]
40.2 nM(Ki)558.4 nM(Ki)

In vitro

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 [H]5-HT or [H]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 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%.


Synonyms

Phenol, 4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]-
4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol
O-Desmethylvenlafaxine
Desvenlafaxine
DVS 233
Pristiq
D-VENIZ
NEWVEN
MDD-XR
O-Desvenlafaxine