Desvenlafaxine Succinate

Catalog No.S4112 Synonyms: WY 45233 Succinate

Desvenlafaxine Succinate Chemical Structure

Molecular Weight(MW): 418.36

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

Size Price Stock Quantity  
In DMSO USD 140 In stock
USD 110 In stock
USD 370 In stock
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Biological Activity

Description Desvenlafaxine Succinate 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

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 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]

Protocol

Animal Research:[1]
+ Expand
  • 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 80 mg/mL (191.22 mM)
Water Insoluble
Ethanol Insoluble
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

* 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 418.36
Formula

C22H24ClN3O.HCl

CAS No. 386750-22-7
Storage powder
in solvent
Synonyms WY 45233 Succinate

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03432221 Not yet recruiting Major Depressive Disorder Corporacion Parc Tauli|Pfizer April 3 2018 --
NCT03432221 Not yet recruiting Major Depressive Disorder Corporacion Parc Tauli|Pfizer April 3 2018 --
NCT02819921 Recruiting Hot Flashes|Breast Neoplasms Seoul National University Hospital|Seoul National University Bundang Hospital|Korea Cancer Center Hospital|Pfizer November 10 2017 Phase 4
NCT02819921 Recruiting Hot Flashes|Breast Neoplasms Seoul National University Hospital|Seoul National University Bundang Hospital|Korea Cancer Center Hospital|Pfizer November 10 2017 Phase 4
NCT02859103 Recruiting Depression|Anhedonia St. Michael''s Hospital Toronto June 1 2017 Phase 4
NCT02859103 Recruiting Depression|Anhedonia St. Michael''s Hospital Toronto June 1 2017 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID