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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters
