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Initial evaluation of 99m T c‐tricarbonyl‐cyclopentadienyl fatty acids derivatives as SPECT tracers for myocardium
Author(s) -
Liu Jianping,
Wang Huan,
Wang Shuxia,
Xue Qianqian,
Wang Dawei,
Wang Hang,
Zhang Huabei
Publication year - 2017
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3497
Subject(s) - chemistry , cyclopentadienyl complex , radiochemistry , organic chemistry , catalysis
Fatty acids are myocardial metabolic agent for detecting myocardial ischemia and infraction. However, no 99m Tc‐labeled fatty acids had potential use in clinical practice. In this study, 99m Tc‐CpTT‐10‐oxo‐para‐PPA ( 1d ), 99m Tc‐CpTT‐11‐oxo‐para‐PPA ( 2d ), 99m Tc‐CpTT‐12‐oxo‐para‐PPA ( 3d ), 99m Tc‐CpTT‐11‐oxo‐ortho‐PPA ( 4d ), and 99m Tc‐CpTT‐11‐oxo‐meta‐PPA ( 5d ) were synthesized by a double ligand transfer reaction, and their biological behaviors were investigated. Compound 2d achieved good heart to blood ratio (3.39 at 5 min after intravenous), and 2d showed high‐heart uptake of 6.20% ID/g at 5 minutes after injection. Compound 3d displayed a prolonged retention in the myocardium (1.43% ID/g at 60 min after injection). Radioactivity accumulation in the lungs, spleen, and blood was eliminated rapidly. In vivo, metabolite analysis presented that compound 6d may be metabolite of 2d through β‐oxidation in tissue. Unfortunately, the biodistribution studies of 1d , 2d , 3d , 4d , and 5d showed fast heart clearance and poor heart to liver ratios, which suggested that the 5 99m Tc‐labeled fatty acid analogues cannot be used for diagnosis.