Title of article
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors
Author/Authors
Junko Tamiya، نويسنده , , Brian Dyck، نويسنده , , Mingzhu Zhang، نويسنده , , Kasey Phan، نويسنده , , Beth A. Fleck، نويسنده , , Anna Aparicio، نويسنده , , Florence Jovic، نويسنده , , Joe A. Tran، نويسنده , , Troy Vickers، نويسنده , , Jonathan Grey، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
3328
To page
3332
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 IC50 values of 1.7 nM at NET and 25 nM at SERT, which were, respectively, 20- and 13-fold more potent than 1S,2R-milnacipran 1–II.
Keywords
Milnacipran , Stereoisomer , Norepinephrine , Serotonin , inhibitor , Lipophilicity , structure–activity relationship , Metabolic stability , permeability , Monoamine transporter
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799555
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