Home Neuronal Signaling Serotonin Transporter inhibitor - Adrenergic Receptor inhibitor Desvenlafaxine For research use only.

Desvenlafaxine

Synonyms: WY 45233 Succinate

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

Desvenlafaxine Chemical Structure

CAS: 93413-62-8

Selleck's Desvenlafaxine has been cited by 1 publication

Purity & Quality Control

Batch: S411301 DMSO] 37 mg/mL] false] Ethanol] 3 mg/mL] false] Water] Insoluble] false Purity: 99.72%
99.72

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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
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
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]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 30 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02637193 Completed
Healthy Subjects
Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer
 December 2015 Phase 1
NCT02200406 Completed
Depression|Opioid Dependence|Methadone Treatment
Centre hospitalier de l''Université de Montréal (CHUM)|Pfizer
 July 2014 Phase 4
NCT00888862 Unknown status
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
Healthy
Wyeth is now a wholly owned subsidiary of Pfizer
 January 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 263.38 Formula

C16H25NO2
CAS No. 93413-62-8 SDF Download Desvenlafaxine SDF
Smiles CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 37 mg/mL ( (140.48 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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