Home Neuronal Signaling Serotonin Transporter inhibitor - Adrenergic Receptor inhibitor Desvenlafaxine

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Desvenlafaxine Serotonin Transporter inhibitor

Cat.No.S4113

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 Serotonin Transporter inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 263.38

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 263.38 Formula

C16H25NO2

 Storage (From the date of receipt)
CAS No. 93413-62-8 Download SDF Storage of Stock Solutions

Synonyms WY 45233 Succinate Smiles CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O

Solubility

In vitro
Batch:

DMSO : 37 mg/mL (140.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Features
Desvenlafaxine is a major active metabolite of venlafaxine.
Targets/IC50/Ki
5-HT [1]
40.2 nM(Ki)
Norepinephrine (NE) [1]
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, this compound inhibits the neuronal uptake of serotonin and norepinephrine. It shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. This chemical inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively.[1] It 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 this agent, which could impact the metabolism of drugs metabolized via this enzyme. [2]
In vivo
Desvenlafaxine rapidly penetrates the male rat brain and hypothalamus. This compound significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. [1] It 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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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