STRUCTURE-ACTIVITY-RELATIONSHIPS OF INHIBITION OF THE DOPAMINE TRANSPORTER BY 3-ARYLBICYCLO[3.2.1]OCTANES

In this report we present an overview of the Structure Activity Relati onships (SAR) which govern the interaction of 3-arylbicyclo[3.2.1]octa nes (tropane analogs) with the dopamine transporter (DAT). Data for in hibition of the DAT by bicyclo[3.2.1]octanes modified at C-2, C-3, C-7 and 8-N are presented and discussed. We postulate that the three dime nsional volume of the bicyclo[3.2.1]octanes influences binding to the DAT and may play a greater role in inhibition of the transporter than does the presence of specific functionality.