Author/Authors :
Ling-Wei Hsin، نويسنده , , Thomas Prisinzano، نويسنده , , Chavon R. Wilkerson، نويسنده , , Christina M. Dersch، نويسنده , , Robert Horel، نويسنده , , Arthur E. Jacobson، نويسنده , , Richard B. Rothman، نويسنده , , Kenner C. Rice، نويسنده ,
Abstract :
A series of optically pure phenyl-and non-phenyl-substituted 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines was synthesized and their binding affinity for dopamine transporter (DAT) was investigated. The analogues with a hydroxyl group in the S configuration were more selective for the DAT over the serotonin transporter (SERT) than the corresponding R enantiomers. Compound (+)-11 showed high affinity and selectivity for DAT over the SERT and, therefore, is a potential candidate for the development of a long-acting cocaine abuse therapeutic agent.
