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ID: ALA1144620
Journal: Bioorg Med Chem Lett
Title: Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3.
Authors: Zheng QH, Gao M, Mock BH, Wang S, Hara T, Nazih R, Miller MA, Receveur TJ, Lopshire JC, Groh WJ, Zipes DP, Hutchins GD, DeGrado TR.
Abstract: The high-affinity choline transporter (CHT1) system is an attractive target for the development of positron emission tomography (PET) biomarkers to probe brain, cardiac, and cancer diseases. An efficient and convenient synthesis of new radiolabeled CHT1 inhibitors [(11)C]hemicholinium-3 and [(18)F]hemicholinium-3 by solid-phase extraction (SPE) technique using a cation-exchange CM Sep-Pak cartridge has been well developed. The preliminary evaluation of both tracers through biodistribution studies in 9L-glioma rats has been performed, and the uptakes in the heart and tumor were observed, while very low brain uptake was seen.
CiteXplore: 17303422