Synthesis and biological activity of some known and putative duloxetine metabolites

Graphic 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 vi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-07, Vol.14 (13), p.3481-3486
Main Authors: Kuo, F., Gillespie, T.A., Kulanthaivel, P., Lantz, R.J., Ma, T.W., Nelson, D.L., Threlkeld, P.G., Wheeler, W.J., Yi, P., Zmijewski, M.
Format: Article
Language:English
Subjects:
Adrenergic Uptake Inhibitors - chemical synthesis
Adrenergic Uptake Inhibitors - metabolism
Adrenergic Uptake Inhibitors - pharmacology
Binding Sites
Biological and medical sciences
Cloning, Molecular
Dopamine Plasma Membrane Transport Proteins
Duloxetine Hydrochloride
Glucuronides - metabolism
Humans
Medical sciences
Membrane Glycoproteins - metabolism
Membrane Transport Proteins - metabolism
Miscellaneous
Models, Chemical
Nerve Tissue Proteins - metabolism
Pharmacology. Drug treatments
Radioligand Assay
Sulfates - metabolism
Thiophenes - chemical synthesis
Thiophenes - metabolism
Thiophenes - pharmacology
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Summary:Graphic 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.04.066