Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3.
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.
Zheng
Qi-Huang
QH
Department of Radiology, Indiana University School of Medicine, Indianapolis, IN 46202, USA. qzheng@iupui.edu
Gao
Mingzhang
M
Mock
Bruce H
BH
Wang
Shuyan
S
Hara
Toshihiko
T
Nazih
Rachid
R
Miller
Michael A
MA
Receveur
Tim J
TJ
Lopshire
John C
JC
Groh
William J
WJ
Zipes
Douglas P
DP
Hutchins
Gary D
GD
DeGrado
Timothy R
TR
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
C501512:CHT1 protein, rat; D002250:Carbon Radioisotopes; D027682:Cation Transport Proteins; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D006426:Hemicholinium 3