Desvenlafaxine

Catalog No.S4113 Synonyms: WY 45233 Succinate

For research use only.

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

Desvenlafaxine Chemical Structure

CAS No. 93413-62-8

Selleck's Desvenlafaxine has been cited by 1 Publication

Purity & Quality Control

Choose Selective Serotonin Transporter Inhibitors

Biological Activity

Description Desvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki 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 [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively.[1] 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. [2]

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. [1] 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%.[2]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 30 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 263.38
Formula

C16H25NO2

CAS No. 93413-62-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02637193 Completed Drug: Venlafaxine|Drug: Moxifloxacin|Drug: Drug - placebo Healthy Subjects Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer December 2015 Phase 1
NCT02200406 Completed Drug: Desvenlafaxine Depression|Opioid Dependence|Methadone Treatment Centre hospitalier de l''Université de Montréal (CHUM)|Pfizer July 2014 Phase 4
NCT00888862 Unknown status Drug: Desvenlafaxine Succinate Major Depressive Disorder|Menopausal Staging and Vasomotor Symptoms (for Females) Hamilton Health Sciences Corporation|Wyeth is now a wholly owned subsidiary of Pfizer|St. Joseph''s Healthcare Hamilton|McMaster University June 2009 Phase 3
NCT00818155 Completed Drug: desvenlafaxine succinate SR|Other: Placebo Healthy Wyeth is now a wholly owned subsidiary of Pfizer January 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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