Synthesis and binding affinities of 2 beta-(3-iodoallyloxycarbonyl)3 beta-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies

Tropane analogues from cocaine, which is known to be one of the most reinfo rcing and addictive compounds, were designed, synthesized, and characterize d for inhibition of presynaptic uptake of dopamine (DA) in brain. Eight new derivatives of 3 beta -aryl-2 beta-(3-iodoallyloxycarbonyl)tropanes were s ynthesized and tested for their potential abilities to displace [H-3]2 beta -carbomethoxy-3 beta-(4-fluorophenyl)tropane (WIN 35,428) binding to the r at striatal membranes. (C) 2001 Elsevier Science Ltd. All rights reserved.