title: Initial evaluation of99mTc-tricarbonyl-cyclopentadienyl fatty acids derivatives as SPECT tracers for myocardium.
abstract: Fatty acids are myocardial metabolic agent for detecting myocardial ischemia and infraction. However, no99mTc-labeled fatty acids had potential use in clinical practice. In this study,99mTc-CpTT-10-oxo-para-PPA (1d),99mTc-CpTT-11-oxo-para-PPA (2d),99mTc-CpTT-12-oxo-para-PPA (3d),99mTc-CpTT-11-oxo-ortho-PPA (4d), and99mTc-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 599mTc-labeled fatty acid analogues cannot be used for diagnosis.
authors.affiliation: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Jianping
authors.identifier: 0000-0003-0087-8414
authors.initials: J
authors.lastname: Liu
authors.affiliation: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Huan
authors.initials: H
authors.lastname: Wang
authors.affiliation: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Shuxia
authors.initials: S
authors.lastname: Wang
authors.affiliation: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Xue
authors.affiliation: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Dawei
authors.initials: D
authors.lastname: Wang
authors.affiliation: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Hang
authors.initials: H
authors.lastname: Wang
authors.affiliation: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Huabei
authors.initials: H
authors.lastname: Zhang
mesh_terms: D000818:Animals; D004355:Drug Stability; D005227:Fatty Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D006321:Heart / Q000000981:diagnostic imaging*; D051379:Mice; D011849:Radioactive Tracers; D011854:Radiochemistry; D013667:Technetium / Q000737:chemistry*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*
chemical_list: D005227:Fatty Acids; D011849:Radioactive Tracers; D013667:Technetium
keywords: SPECT tracers; fatty acid; myocardial imaging; β-oxidation