title: Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging.
abstract: Acebutolol was successfully labeled with (125) I via direct electrophilic substitution reaction. Radioiodinated acebutolol was prepared with a maximum radiochemical yield of 96.5 ± 0.3% and in vitro stability up to 72 h. The in vivo biological distribution of radioiodinated acebutolol showed high heart uptake of 37.8 ± 0.14% injected activity/g organ with low lungs and liver uptakes at 5 min post-injection. In vivo receptor blocking study was carried out in mice to evaluate its selectivity to heart. Radioiodinated acebutolol showed fast heart accumulation with high heart/liver ratio, which provides the ability for fast myocardial imaging with significant decrease in the radiation hazards risk on patients. So, radioiodinated acebutolol could be displayed as a radiotracer drug of choice in case of emergency patients for myocardial perfusion imaging.
authors.affiliation: Labeled Compound Department, Hot Labs Center, Atomic Energy Authority, PO13759, Cairo, Egypt.
authors.forename: M M
authors.initials: MM
authors.lastname: Swidan
authors.forename: T M
authors.initials: TM
authors.lastname: Sakr
authors.forename: M A
authors.initials: MA
authors.lastname: Motaleb
authors.forename: A Abd
authors.initials: AA
authors.lastname: El-Bary
authors.forename: M T
authors.initials: MT
authors.lastname: El-Kolaly
mesh_terms: D000070:Acebutolol / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D000818:Animals; D007457:Iodine Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D051379:Mice; D055414:Myocardial Perfusion Imaging / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D000070:Acebutolol
keywords: acebutolol; chloramin-T; myocardial perfusion imaging; radioiodination