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• W2087127914 abstract "N-demethylation of the selective serotonin reuptake inhibitor sertraline to desmethylsertraline yields a compound with 10- to 20-fold less potency at blocking serotonin (5-HT) reuptake as measured in vitro. In the present study desmethylsertraline (DMS) was examined in two in vivo models of reuptake inhibition—elevation of extracellular 5-HT in the corpus striatum as measured by microdialysis and inhibition of firing of serotonin-containing dorsal raphe neurons. Whereas sertraline (1, 3.2, and 10 mg/kg SC) produced a dose-dependent increase in extracellular 5-HT and a decrease in 5-HIAA in rat striatum, desmethylsertraline was without effect on either parameter. In similar fashion, desmethylsertraline had no effect on dorsal raphe cell firing at a dose (1,000 μg/kg IV) nearly 20-fold the ED50 for sertraline (52 μg/kg). Taken together, these data suggest that DMS does not contribute to the blockade of central 5-HT reuptake produced by sertraline in vivo and therefore would be expected to play a negligible role in its clinical activity." @default.
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• W2087127914 date "1996-04-01" @default.
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• W2087127914 title "Comparison of the Effects of Sertraline and Its Metabolite Desmethylsertraline on Blockade of Central 5-HT Reuptake In Vivo" @default.
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• W2087127914 doi "https://doi.org/10.1016/0893-133x(95)00112-q" @default.
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