title: Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3.
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.
authors.affiliation: Department of Radiology, Indiana University School of Medicine, Indianapolis, IN 46202, USA. qzheng@iupui.edu
authors.forename: Qi-Huang
authors.initials: QH
authors.lastname: Zheng
authors.forename: Mingzhang
authors.initials: M
authors.lastname: Gao
authors.forename: Bruce H
authors.initials: BH
authors.lastname: Mock
authors.forename: Shuyan
authors.initials: S
authors.lastname: Wang
authors.forename: Toshihiko
authors.initials: T
authors.lastname: Hara
authors.forename: Rachid
authors.initials: R
authors.lastname: Nazih
authors.forename: Michael A
authors.initials: MA
authors.lastname: Miller
authors.forename: Tim J
authors.initials: TJ
authors.lastname: Receveur
authors.forename: John C
authors.initials: JC
authors.lastname: Lopshire
authors.forename: William J
authors.initials: WJ
authors.lastname: Groh
authors.forename: Douglas P
authors.initials: DP
authors.lastname: Zipes
authors.forename: Gary D
authors.initials: GD
authors.lastname: Hutchins
authors.forename: Timothy R
authors.initials: TR
authors.lastname: DeGrado
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes; D027682:Cation Transport Proteins / Q000037:antagonists & inhibitors*; D005462:Fluorine Radioisotopes; D005910:Glioma / Q000175:diagnosis / Q000378:metabolism; D006426:Hemicholinium 3 / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D009206:Myocardium / Q000378:metabolism; D049268:Positron-Emission Tomography / Q000379:methods; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats
chemical_list: C501512:CHT1 protein, rat; D002250:Carbon Radioisotopes; D027682:Cation Transport Proteins; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D006426:Hemicholinium 3