title: Novel synthesis and initial preclinical evaluation of (18)F-[FDG] labeled rhodamine: a potential PET myocardial perfusion imaging agent.
abstract: Myocardial perfusion imaging is one of the most commonly performed investigations in nuclear medicine studies. Due to the clinical importance of [(18)F]-fluoro-2-deoxy-D-glucose ([(18)F]-FDG) and its availability in almost every PET center, a new radiofluorinated [(18)F]-FDG-rhodamine conjugate was synthesized using [(18)F]-FDG as a prosthetic group. In a convenient and simple one-step radiosynthesis, [(18)F]-FDG-rhodamine conjugate was prepared in quantitative radiochemical yields, with total synthesis time of nearly 20 min and radiochemical purity of greater than 98%, without the need for HPLC purification, which make these approaches amenable for automation. Biodistribution studies in normal rats at 60 min post-injection demonstrated a high uptake in the heart (>11% ID/g) and favorable pharmacokinetics. Additionally, [(18)F]-FDG-rhodamine showed an extraction value of 27.63%±5.12% in rat hearts. These results demonstrate that [(18)F]-FDG-rhodamine conjugate may be useful as an imaging agent for the positron emission tomography evaluation of myocardial perfusion.
authors.affiliation: Cyclotron and Radiopharmaceuticals and Cell Biology Departments, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Kingdom of Saudi Arabia. Electronic address: jammaz@kfshrc.edu.sa.
authors.forename: Ibrahim
authors.initials: I
authors.lastname: AlJammaz
authors.affiliation: Cyclotron and Radiopharmaceuticals and Cell Biology Departments, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Kingdom of Saudi Arabia.
authors.forename: Basim
authors.initials: B
authors.lastname: Al-Otaibi
authors.affiliation: Cyclotron and Radiopharmaceuticals and Cell Biology Departments, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Kingdom of Saudi Arabia.
authors.forename: Hussein
authors.initials: H
authors.lastname: AlHindas
authors.affiliation: Cyclotron and Radiopharmaceuticals and Cell Biology Departments, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Kingdom of Saudi Arabia.
authors.forename: Subhani M
authors.initials: SM
authors.lastname: Okarvi
mesh_terms: D000818:Animals; D060326:Chemistry Techniques, Synthetic; D004355:Drug Stability; D019788:Fluorodeoxyglucose F18 / Q000737:chemistry*; D006801:Humans; D008297:Male; D055414:Myocardial Perfusion Imaging / Q000379:methods*; D009206:Myocardium / Q000378:metabolism; D049268:Positron-Emission Tomography / Q000379:methods*; D011854:Radiochemistry; D051381:Rats; D012235:Rhodamines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D012235:Rhodamines; D019788:Fluorodeoxyglucose F18
keywords: FDG; Fluorine-18; Myocardial perfusion imaging; Positron emission tomography; Rhodamine