Desvenlafaxine

Catalog No.S4113 Synonyms: WY 45233 Succinate

Desvenlafaxine Chemical Structure

Molecular Weight(MW): 263.38

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

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 60 In stock
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Biological Activity

Description Desvenlafaxine 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

Animal Research:[1]
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  • Animal Models: Male Sprague-Dawley rats
  • Formulation: 0.25% Tween 80 and 0.5% methylcellulose
  • Dosages: 30 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 37 mg/mL (140.48 mM)
Ethanol 3 mg/mL (11.39 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
0.5% methylcellulose+0.2% Tween 80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 263.38
Formula

C16H25NO2

CAS No. 93413-62-8
Storage powder
Synonyms WY 45233 Succinate

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02859103 Not yet recruiting Depression|Anhedonia St. Michaels Hospital, Toronto November 2016 Phase 4
NCT02819921 Not yet recruiting Hot Flashes|Breast Neoplasms Seoul National University Hospital|Seoul National University Bundang Hospital|Korea Cancer Center Hospital|Pfizer September 2016 Phase 4
NCT02330679 Unknown status Major Depressive Disorder University of Calgary|University of Alberta December 2014 Phase 4
NCT02200406 Recruiting Depression|Opioid Dependence|Methadone Treatment Didier Jutras-Aswad|Pfizer|Centre hospitalier de lUniversité de Montréal (CHUM) July 2014 Phase 4
NCT01974934 Recruiting Vascular Depression Hotel-Dieu Grace Healthcare December 2013 Phase 4
NCT01977378 Unknown status Major Depressive Disorder Jiangsu Hansoh Pharmaceutical Co., Ltd. October 2013 Phase 2|Phase 3

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