Synthesis and biological activity of some known and putative duloxetine metabolites.
Article Details
- CitationCopy to clipboard
Kuo F, Gillespie TA, Kulanthaivel P, Lantz RJ, Ma TW, Nelson DL, Threlkeld PG, Wheeler WJ, Yi P, Zmijewski M
Synthesis and biological activity of some known and putative duloxetine metabolites.
Bioorg Med Chem Lett. 2004 Jul 5;14(13):3481-6.
- PubMed ID
- 15177457 [ View in PubMed]
- Abstract
Several putative phase I duloxetine metabolites, 4-hydroxy-, 5-hydroxy-, 6-hydroxy-, 5-hydroxy-6-methoxy-, 6-hydroxy-5-methoxy-, 5,6-dihydroxy-, and 4,6-dihydroxyduloxetine were synthesized, and their phase II metabolite as glucuronide or sulfate conjugates were also synthesized. Their in vitro binding activities were compared to that of parent compound duloxetine.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Duloxetine Sodium-dependent dopamine transporter Ki (nM) 240000 N/A N/A Details Duloxetine Sodium-dependent noradrenaline transporter Ki (nM) 7450 N/A N/A Details Duloxetine Sodium-dependent serotonin transporter Ki (nM) 790 N/A N/A Details