Title of article
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors
Author/Authors
Troy Vickers، نويسنده , , Brian Dyck، نويسنده , , Junko Tamiya، نويسنده , , Mingzhu Zhang، نويسنده , , Florence Jovic، نويسنده , , Jonathan Grey، نويسنده , , Beth A. Fleck، نويسنده , , Anna Aparicio، نويسنده , , Michael Johns، نويسنده , , Liping Jin، نويسنده , , Hui Tang، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
3230
To page
3235
Abstract
A series of milnacipran analogs containing a heteroaromatic group were synthesized and studied as monoamine transporter inhibitors. Many compounds exhibited higher potency than milnacipran at NET and NET/SERT with no significant change in lipophilicity. For example, compound R-26f was about 10-fold more potent than milnacipran with IC50 values of 8.7 and 26 nM at NET and SERT, respectively.
Keywords
Potency , Lipophilicity , Milnacipran , Monoamine transporter inhibitor , Metabolic stability , Clearance
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799536
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