Desvenlafaxine Succinate hydrate

Synonyms: WY 45233 Succinate

Desvenlafaxine Succinate hydrate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.

Desvenlafaxine Succinate hydrate Chemical Structure

Desvenlafaxine Succinate hydrate Chemical Structure

CAS: 386750-22-7

Selleck's Desvenlafaxine Succinate hydrate has been cited by 1 publication

Purity & Quality Control

Batch: S411201 DMSO] 80 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.96%
99.96

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Biological Activity

Description Desvenlafaxine Succinate hydrate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.
Features A major active metabolite of venlafaxine.
Targets
5-HT [1] Norepinephrine (NE) [1]
40.2 nM(Ki) 558.4 nM(Ki)
In vitro
In vitro

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.[1] 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. [2]

In Vivo
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. [1] 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%.[2]

Animal Research Animal Models Male Sprague-Dawley rats
Dosages 30 mg/kg
Administration Oral

Chemical Information & Solubility

Molecular Weight 399.48 Formula

C16H25NO2.C4H6O4.H2O

CAS No. 386750-22-7 SDF Download Desvenlafaxine Succinate hydrate SDF
Smiles CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (200.26 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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