Synthesis of 2 beta-acyl-3 beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites

A series of 3 beta -naphthyltropane derivatives were synthesized and found to show high affinity at both the dopamine and serotonin transporter sites, leading to some of the most potent inhibitors known based on the tropane s tructure. Comparative molecular field analysis (CoMFA) models were develope d for both dopamine and serotonin transporter binding data. These models pr ovide insights into those factors that influence binding at the two transpo rters.