Novel approach using [18F]FTHA-PET and de novo synthesized VLDL for assessment of FFA metabolism in a rat model of diet induced NAFLD

A Fully Automated Synthesis of 14-(R,S)-[18F]fluoro-6-thia-heptadecanoic Acid ([18F]FTHA) on the Elixys Radiosynthesizer

“…To this end, the constant successful chemical quality control results after all syntheses ( Table 2 ) confirm the reliability of the synthesis. Our preclinical study [ 11 ] has not recorded any difference in the blood uptake and imaging with [ 18 F]FTHA produced on either module. Additionally, the automated production in the cassette-based Elixys radiosynthesizer can positively affect clinical studies investigating FFA alterations, as multiple clinical doses could be produced in one synthesis.…”

“…The versatility and applicability of covalently bound radionuclides are vast, especially as the chemical structure is not ( 11 C) or only slightly ( 18 F) altered compared to PET tracers with a metal-based radiolabel [2]. For instance, [1- 11 C]palmitate can be used as a free fatty acid analogue without changing its biochemical properties [3]. However, the short half-life of the isotope and 11 C-carrying metabolites (especially [ 11 C]CO 2 and [ 11 C]HCO 3 − ) require an increased dosage for metabolic studies of patients and necessitate the assessment of the input function through blood sampling.…”

“…For instance, [1- 11 C]palmitate can be used as a free fatty acid analogue without changing its biochemical properties [3]. However, the short half-life of the isotope and 11 C-carrying metabolites (especially [ 11 C]CO 2 and [ 11 C]HCO 3 − ) require an increased dosage for metabolic studies of patients and necessitate the assessment of the input function through blood sampling. Hence, significant efforts to improve labelling efficiency were made in the last decade to address the growing importance of nucleophilic 18 F-fluorination chemistry [4].…”

“…Hence, significant efforts to improve labelling efficiency were made in the last decade to address the growing importance of nucleophilic 18 F-fluorination chemistry [4]. With a half-life of 109.7 min, fluorine-18 is more convenient for tracer production and the exploration of metabolic pathways, avoiding the release of 11 C-metabolites into the circulatory system.…”

“…The liver and adipose tissue are the main lipogenic tissues. Recent studies show a revival of interest in FFA metabolism, with the application of adipose tissue function [9,10], obesity [11][12][13], and type 2 diabetes [14,15]. The [ 18 F]FTHA tracer synthesis was developed in 1991 by DeGrado [16].…”