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 ,
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
