PMID: 7535937Jan 1, 1995Paper

Comparison of desmethylsertraline with sertraline as a monoamine uptake inhibitor in vivo

Progress in Neuro-psychopharmacology & Biological Psychiatry
R W FullerJ E Audia

Abstract

1. Desmethylsertraline, a metabolite of the antidepressant drug sertraline, was compared with sertraline for its ability to produce effects characteristic of inhibitors of the serotonin transporter in vivo. Desmethylsertraline antagonized brain serotonin depletion by p-chloroamphetamine, a depletion dependent upon the serotonin transporter, being less potent than sertraline in rats but almost as potent as sertraline in mice. Desmethylsertraline was a weak antagonist of 6-hydroxydopamine-induced depletion of heart norepinephrine in mice; sertraline had no effect at the doses studied. 2. Desmethylsertraline decreased brain concentrations of 5-hydroxyindoleacetic acid (5HIAA) in rats as did sertraline, the duration of the effect after both drugs being at least 24 hrs but less than 48 hrs. 3. After sertraline injection, desmethylsertraline was present in rat brain at higher concentrations than the parent drug at 8 hrs and thereafter. 4. In rats, repeated injections of sertraline, at doses previously shown to diminish beta-adrenergic receptor-mediated responses, led to marked accumulation of desmethylsertraline in brain and to inhibition of the catecholamine transporters. 5. In mice, brain concentrations of desmethylsertraline were ...Continue Reading

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Citations

Oct 12, 2010·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Myung Joo KangJaehwi Lee
May 19, 2004·Proceedings of the National Academy of Sciences of the United States of America·John F CryanIrwin Lucki
Dec 2, 2010·Biomedical Chromatography : BMC·Alina Plenis, Tomasz Bączek
Dec 19, 2019·Pharmacogenetics and Genomics·Rachel HuddartTeri E Klein
Nov 10, 1998·Journal of Psychopharmacology·P J Goodnick, B J Goldstein

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