Synthesis and biological activity of some known and putative duloxetine metabolites

F Kuo, TA Gillespie, P Kulanthaivel, RJ Lantz…

Index: Kuo; Gillespie; Kulanthaivel; Lantz; Ma; Nelson; Threlkeld; Wheeler; Yi; Zmijewski Bioorganic and Medicinal Chemistry Letters, 2004 ,  vol. 14,  # 13  p. 3481 - 3486

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Citation Number: 50

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.