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Design, Synthesis, and Evaluation of Fluorinated Radioligands for Myelin Imaging.

A. Tiwari,Chunying Wu,Junqing Zhu,S. Zhang,Jinle Zhu,William R. Wang,Jinming Zhang,C. Tatsuoka,P. Matthews,Robert H Miller,Yanming Wang

Published 2016 in Journal of Medicinal Chemistry

ABSTRACT

Myelination is one of the fundamental processes in vertebrates. A major challenge is to quantitatively image myelin distribution in the central nervous system. For this reason, we designed and synthesized a series of fluorinated radioligands that can be radiolabeled as radiotracers for positron emission tomography (PET) imaging of myelin. These newly developed radioligands readily penetrate the blood-brain barrier and selectively bind to myelin membranes in the white matter region. Structure-activity relationship studies of such ligands suggested that optimal permeability could be achieved with calculated lipophilicty in the range of 3-4. After radiolabeling with fluorine-18, the brain uptake and retention of each radioligand were determined by microPET/CT imaging studies. These pharmacokinetic studies led us to identify a lead compound ([(18)F]FMeDAS, 32) with promising in vivo binding properties, which was subsequently validated by ex vivo autoradiography.

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