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, 18 (11), 3328-32

Identification of 1S,2R-milnacipran Analogs as Potent Norepinephrine and Serotonin Transporter Inhibitors

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Identification of 1S,2R-milnacipran Analogs as Potent Norepinephrine and Serotonin Transporter Inhibitors

Junko Tamiya et al. Bioorg Med Chem Lett.

Abstract

A series of milnacipran analogs were synthesized and studied as monoamine transporter inhibitors, and several potent compounds with moderate lipophilicity were identified from the 1S,2R-isomers. Thus, 15l exhibited IC(50) values of 1.7nM at NET and 25nM at SERT, which were, respectively, 20- and 13-fold more potent than 1S,2R-milnacipran 1-II.

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