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 (K i = 76 nM vs. 3 nM, respectively), but conversely, is more balanced as a monoamine reuptake inhibitor (5-HT (K i ) = 76 nM; NE (K i ) = 420 nM; DA (K i ) = 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.[1]
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.
See also
References
^ Wong DT, Bymaster FP, Engleman EA (1995). "Prozac (fluoxetine, Lilly 110140), the first selective serotonin uptake inhibitor and an antidepressant drug: twenty years since its first publication". Life Sci . 57 (5): 411–41. doi :10.1016/0024-3205(95)00209-o . PMID 7623609 .
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