Desvenlafaxine Succinate 386750-22-7

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Molecular Weight:


381.46 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.





Biological Activity

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.


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.


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.


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%.

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Product Categories : Neuronal Signaling > 5-HT Receptor Inhibitor