An active metabolite of venlafaxine; inhibits NET and SERT (IC50s = 47.3 and 531.3 nM

Desvenlafaxine (succinate hydrate) – 25 mg

Brand:
Cayman
CAS:
386750-22-7
Storage:
-20
UN-No:
Non-Hazardous - /

Desvenlafaxine is an active metabolite of the selective norepinephrine and serotonin reuptake inhibitor (SNRI) venlafaxine.{32153} It is formed from venlafaxine by the cytochrome P450 (CYP) isoform CYP2D6.{32155} Desvenlafaxine inhibits the norepinephrine transporter (NET) and serotonin transporter (SERT) with IC50 values of 47.3 and 531.3 nM, respectively, for the human transporters.{32153} It is selective for NET and SERT over 50 receptors, peptides, and ion channels among others. It increases extracellular norepinephrine (NE) in the male rat hypothalamus and increases extracellular serotonin (5-HT) in the same region when used in combination with the 5-HT1A receptor antagonist WAY-100635 (Item No. 14599). Desvenlafaxine (3 mg/kg per day) reduces the time rats spend immobile in the forced swim test in a rat model of cognitive deficits and depression induced by myocardial infarction (MI) when compared with MI-vehicle control animals 16 weeks following MI.{48908} It also improves learning in the passive avoidance step-down test two weeks following MI compared to MI-vehicle control rats and spatial memory in the Morris water maze 16 weeks following MI.  

 

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Description

An active metabolite of venlafaxine; inhibits NET and SERT (IC50s = 47.3 and 531.3 nM, respectively); selective for NET and SERT over 50 non-transporter targets; increases extracellular NE in the male rat hypothalamus and 5-HT in the same region when used in combination with WAY-100635; reduces the time rats spend immobile in the forced swim test in a rat model of cognitive deficits and depression induced by MI when compared with MI-vehicle control animals 16 weeks following MI; improves learning in the passive avoidance step-down test two weeks following MI compared to MI-vehicle control rats and spatial memory in the Morris water maze 16 weeks following MI

Formal name: butanedioic acid, compd. with 4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol, hydrate (1:1:1)

Synonyms:  O-Desmethyl Venlafaxine

Molecular weight: 399.5

CAS: 386750-22-7

Purity: ≥98%

Formulation: A solid

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