Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents

X Peng, A Zhang, NS Kula, RJ Baldessarini…

Index: Peng, Xuemei; Zhang, Ao; Kula, Nora S.; Baldessarini, Ross J.; Neumeyer, John L. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5635 - 5639

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Citation Number: 12

Abstract

A series of novel fluoroalkyl-containing tropane derivatives (6–8, 10–14, 17, and 18) were synthesized from cocaine. Novel compounds were evaluated for affinity and selectivity in competitive radioligand binding assays selective for cerebral serotonin (5-HT), dopamine (DA), and norepinephrine (NE) transporters (SERT, DAT, and NET). The nortropane- fluoroalkyl esters (7, 10, 11) were most potent for SERT (Ki: 0.18, 0.24, and 0.30 nM, ...