Synthesis and biological activity of some known and putative duloxetine metabolites.

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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

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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