Synthesis, Fluorine-18 Radiolabeling, and Biological Evaluation of N-((E)-4-Fluorobut-2-en-1-yl)-2β-carbomethoxy-3β-(4′-halophenyl) nortropanes: Candidate …

JS Stehouwer, LM Daniel, P Chen, RJ Voll…

Index: Stehouwer, Jeffrey S.; Daniel, Lauryn M.; Chen, Ping; Voll, Ronald J.; Williams, Larry; Plott, Susan J.; Votaw, John R.; Owens, Michael J.; Howell, Leonard; Goodman, Mark M. Journal of Medicinal Chemistry, 2010 , vol. 53, # 15 p. 5549 - 5557

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Citation Number: 12

Abstract

The N-(E)-fluorobutenyl-3β-(para-halo-phenyl) nortropanes 9− 12 were synthesized as ligands of the dopamine transporter (DAT) for use as 18F-labeled positron emission tomography (PET) imaging agents. In vitro competition binding assays demonstrated that compounds 9− 12 have a high affinity for the DAT and are selective for the DAT compared to the serotonin and norepinephrine transporters. MicroPET imaging with [18F] 9−[18F] 11 in ...