Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[aryl or heteroaryl]phenyltropanes |
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| Authors: | Tamagnan Gilles Alagille David Fu Xing Kula Nora S Baldessarini Ross J Innis Robert B Baldwin Ronald M |
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| Institution: | Department of Psychiatry, Yale University and VA CT HCS/116A2, 950 Campbell Avenue, West Haven, CT 06516, USA. gtamagnan@indd.org |
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| 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. |
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