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ID: ALA1148559

Journal: Bioorg Med Chem Lett

Title: Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[aryl or heteroaryl]phenyltropanes.

Authors: Tamagnan G, Alagille D, Fu X, Kula NS, Baldessarini RJ, Innis RB, Baldwin RM.

Abstract: A series of 16 new 2beta-carbomethoxy-3beta-[aryl or heteroaryl]phenyltropane derivatives was synthesized and evaluated for binding to monoamine transporters. Most of the compounds exhibited nanomolar affinity for the serotonin transporter (SERT). Four compounds presented a particularly attractive pharmacological profile, with very high SERT affinity (K(i) 0.15-0.5 nM) and selectivity versus the dopamine transporter of 25- to 77-fold.

CiteXplore: 16236497

DOI: 10.1016/j.bmcl.2005.09.016