Open AccessSynthesis and evaluation of radiogallium-labeled long-chain fatty acid derivatives as myocardial metabolic imaging agents
Author(s) -
Nurmaya Effendi,
Kenji Mishiro,
Hiroshi Wakabayashi,
Malwina Gabryel-Skrodzka,
Kazuhiro Shiba,
Junichi Taki,
Renata Jastrząb,
Seigo Kinuya,
Kenji Ogawa
Publication year - 2021
Publication title -
plos one
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.99
H-Index - 332
ISSN - 1932-6203
DOI - 10.1371/journal.pone.0261226
Subject(s) - chemistry , fatty acid , biochemistry
Since long-chain fatty acids work as the primary energy source for the myocardium, radiolabeled long-chain fatty acids play an important role as imaging agents to diagnose metabolic heart dysfunction and heart diseases. With the aim of developing radiogallium-labeled fatty acids, herein four fatty acid-based tracers, [ 67 Ga]Ga-HBED-CC-PDA, [ 67 Ga]Ga-HBED-CC-MHDA, [ 67 Ga]Ga-DOTA-PDA, and [ 67 Ga]Ga-DOTA-MHDA, which are [ 67 Ga]Ga-HBED-CC and [ 67 Ga]Ga-DOTA conjugated with pentadecanoic acid (PDA) and 3-methylhexadecanoic acid (MHDA), were synthesized, and their potential for myocardial metabolic imaging was evaluated. Those tracers were found to be chemically stable in 0.1 M phosphate buffered saline. Initial [ 67 Ga]Ga-HBED-CC-PDA, [ 67 Ga]Ga-HBED-CC-MHDA, [ 67 Ga]Ga-DOTA-PDA, and [ 67 Ga]Ga-DOTA-MHDA uptakes in the heart at 0.5 min postinjection were 5.01 ± 0.30%ID/g, 5.74 ± 1.02%ID/g, 5.67 ± 0.22%ID/g, and 5.29 ± 0.10%ID/g, respectively. These values were significantly lower than that of [ 123 I]BMIPP (21.36 ± 2.73%ID/g). For their clinical application as myocardial metabolic imaging agents, further structural modifications are required to increase their uptake in the heart.