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Synthesis of 2β-Acyl-3β-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and Their Binding Affinities at Dopamine and Serotonin Transport Sites

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journal contribution
posted on 12.04.2001, 00:00 by Huw M. L. Davies, Vernon Gilliatt, Lisa A. Kuhn, Elie Saikali, Pingda Ren, Philip S. Hammond, Tammy Sexton, Steven R. Childers
A series of 3β-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 structure. Comparative molecular field analysis (CoMFA) models were developed for both dopamine and serotonin transporter binding data. These models provide insights into those factors that influence binding at the two transporters.