Kalpana Kalpana (Editor)

Desmethylsertraline

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ATC code
  
none

Excretion
  
urine

PubChem CID
  
114743

Biological half-life
  
66 hours

CAS Number
  
87857-41-8

Molar mass
  
292.2 g/mol

Desmethylsertraline httpsuploadwikimediaorgwikipediacommonsthu

Legal status
  
In general: uncontrolled

Desmethylsertraline (DMS), also known as norsertraline, is an active metabolite of the antidepressant drug sertraline. Like sertraline, desmethylsertraline acts as a monoamine reuptake inhibitor, and may be responsible for some of its parent's therapeutic benefits. However, DMS is significantly less potent relative to sertraline as a serotonin reuptake inhibitor (Ki = 76 nM vs. 3 nM, respectively), but conversely, is more balanced as a monoamine reuptake inhibitor (5-HT (Ki) = 76 nM; NE (Ki) = 420 nM; DA (Ki) = 440 nM), which has the effective result of DMS contrarily behaving as a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with about 5.5-fold preference for inhibiting serotonin reuptake relative to catecholamine reuptake.

Dasotraline, a stereoisomer of DMS, is also an SNDRI, and has been investigated for the potential clinical treatment of major depressive disorder, attention-deficit disorder, and eating disorders, but has not been approved or marketed for any indication.

References

Desmethylsertraline Wikipedia


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