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.

Adaptation of hard gelatin capsules for oral delivery of aqueous radiopharmaceuticals

“…The indicated radionuclidic and radiochemical purity of I −131 product solution >99.9%, Figs. 7 and 8, are totally matching with the accepted criteria of pharmacopeia proving its safe use for human [37,38].…”

New quinoxaline compounds as DPP-4 inhibitors and hypoglycemics: design, synthesis, computational and bio-distribution studies

“…This leads to the DPP-4 suppression effect, blocking the inactivation of the incretin hormones with the consequent stimulation of insulin secretion and inhibition of glucagon secretion, leading to the control of the glucose level in the body. [75][76][77][78][79][80][81][82][83] In addition, it was clear that the excretion pathway of the 131 I-SQ compound is through the renal route. Moreover, it did not show any high accumulation in other body organs.…”

Amelioration of Tumor Targeting and In Vivo Biodistribution of 99mTc-Methotrexate-Gold Nanoparticles (99mTc-Mex-AuNPs)

“…The in vitro stability of 99m Tc-Mex-AuNPs was performed to evaluate its stability in physiological media, the feasibility of further in-vivo evaluations studies and confirming its suitability to be a physiologically stable nano-probe. 35 Exactly 100 ml of the 99m Tc-Mex-AuNPs was incubated with 900 ml of normal mice serum for 24 h at 37 °C.…”