Desvenlafaxine Succinate: A New Serotonin and Norepinephrine Reuptake Inhibitor
@article{Deecher2006DesvenlafaxineSA, title={Desvenlafaxine Succinate: A New Serotonin and Norepinephrine Reuptake Inhibitor}, author={Darlene C. Deecher and Chad E. Beyer and Grace H. Johnston and Jenifer A. Bray and S. Shah and Magid A Abou-Gharbia and Terrance H. Andree}, journal={Journal of Pharmacology and Experimental Therapeutics}, year={2006}, volume={318}, pages={657 - 665} }
The purpose of this study was to characterize a new chemical entity, desvenlafaxine succinate (DVS). DVS is a novel salt form of the isolated major active metabolite of venlafaxine. Competitive radioligand binding assays were performed using cells expressing either the human serotonin (5-HT) transporter (hSERT) or norepinephrine (NE) transporter (hNET) with Ki values for DVS of 40.2 ± 1.6 and 558.4 ± 121.6 nM, respectively. DVS showed weak binding affinity (62% inhibition at 100 μM) at the…
208 Citations
Desvenlafaxine Succinate Identifies Novel Antagonist Binding Determinants in the Human Norepinephrine Transporter
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It is documented that Val148 in hNET transmembrane domain 3 selectively disrupts NIS binding but not that of DVS, and these differences seem not to arise from preparation-specific perturbations of ligand intrinsic affinity or antagonist-specific surface trafficking but rather from protein conformational alterations that perturb the relationships between distinct hNET binding sites.
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Investigation of the effects of LPM570065 on extracellular 5-HT, DA and NE levels in the rat striatum after acute and chronic administration relative to desvenlafaxine suggests that LPM 570065 may have greater efficacy and/or a more rapid onset of antidepressant action than desVENlafAXine and also counterbalance the harmful effects of desvenLafaxines.
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Desvenlafaxine : Frequently Asked Questions
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Since February 2008 when desvenlafaxine first came to market, clinicians have wondered about the differences between this new antidepressant and venlafAXine extended release (ER).
Desvenlafaxine succinate for major depressive disorder: a critical review of the evidence
- Psychology, BiologyExpert review of neurotherapeutics
- 2008
DVS is a useful addition to the options available for the treatment of MDD in light of the limited efficacy of currently available antidepressants and its simple metabolism, lower risk of drug–drug interactions and lack of need for extensive titration to achieve therapeutic efficacy.
Desvenlafaxine Succinate: A Newer Antidepressant for the Treatment of Depression and Somatic Symptoms
- Medicine, PsychologyPostgraduate medicine
- 2010
Current evidence indicates that DVS has proven efficacy, acceptable safety and tolerability profiles, convenient dosing, and minimal impact on the cytochrome P450 enzyme system, which is a potential advantage over other selective serotonin noradrenaline reuptake inhibitors.
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