Stan Penglis

99mTc-Alafosfalin: an antibiotic peptide infection imaging agent

The radiolabeled antibiotic peptide (99m)Tc-alafosfalin was assessed as an infection imaging agent in a rat model by comparison with (99m)Tc-DTPA and (99m)Tc-leukocytes. (99m)Tc-alafosfalin was prepared via an instant cold kit and (99m)Tc-leukocytes were prepared using (99m)Tc-stannous fluoride colloid in an ex vivo labeling procedure of whole blood. In separate experiments, the three radiotracers were administered to rats infected with staphylococcus aureus. Quantitative biodistribution studies were performed as well as scintigraphic images and histopathology. (99m)Tc-alafosfalin is a stable product, obtained in high radiochemical purity (>95%). This agent was mainly renally excreted, with low liver, spleen and bone uptake, and resulted in a mean ratio of infected/non-infected thighs of 4.3/1.0 at 4 hr post radiotracer injection. (99m)Tc-DTPA gave a corresponding ratio of 1.9/1.0 and (99m)Tc-leukocytes gave 20.0/1.0 at the same time point. An in vitro assay found the level of (99m)Tc-alafosfalin binding to staphylococcus aureas higher than (99m)Tc-DTPA (10% versus 1% respectively). (99m)Tc-alafosfalin accumulates at sites of infection in a rat model better than the perfusion molecule (99m)Tc-DTPA, yet less than (99m)Tc-leukocytes. The distribution characteristics of this (99m)Tc-antibiotic peptide would be an advantage in imaging abdominal and soft tissue infection.

Radiolabeling and biodistribution of amiodarone and desethylamiodarone.

The antiarrhythmic drug amiodarone and its metabolite desethylamiodarone, were radiolabeled with sodium [123I]-iodide in > 98% yield using the exchange labeling method. Biodistribution studies with 123I-amiodarone in mice showed high liver and lung uptake. Heart uptake of 0.98% of the injected dose (id) peaked at 5 min, with clearance seen over 60 min to 0.44% id. 123I-Desethylamiodarone (123I-DEA) showed heart uptake of 0.58% id peaking at 5 min, with slower clearance seen over 60 min to 0.43% id. These results indicate that both agents have poor selectivity as myocardial imaging tracers. Low 123I-DEA brain uptake at 5 min (0.49% id) and rapid washout after 60 min indicate that 123I-desethylamiodarone has limited application as a brain imaging agent.

The Preparation of 99mTc—Tertiarybutylisonitrile (99mTc-TBI) by a method suitable for routine clinical use

The myocardial imaging agent technetium-99m-hexakis (tertiarybutylisonitrile) (99mTc-TBI) was prepared by the reaction of [99mTc]pertechnetate with TBI in 50% ethanol/0.9% saline at 100 degrees C, using stannous chloride as the reducing agent. A study of the reaction parameters enabled the yield to be optimized to better than 90%, although this was reduced to approximately 60% if a purification step was carried out. Chromatographic analysis on ITLC-SG medium showed the final product to be of high radiochemical purity. Biological studies comprising biodistribution in mice over a 2-h period, imaging studies in animals and sub-acute toxicity testing in mice indicated that 99mTc-TBI prepared as here described is a suitable agent for routine clinical use in humans.

Radiochemical characterization of modified technegas

The aim of this study was to characterize modified Technegas, employing radiochemical analyses and qualitative rabbit organ imaging techniques. Electrophoresis, thin layer chromatography and imaging studies, found modified Technegas to behave like sodium [99mTc]pertechnetate (pertechnetate). Our data indicate that modified Technegas is a pertechnetate aerosol, which results from the presence of 3% oxygen in the reaction atmosphere of the Technegas generator.

The effect of lipophilic substituents on the biological properties of EDTA complexes containing paramagnetic metal ions

Complexes of the radioactive paramagnetic metal ions 51Cr(III), 54Mn(II), 59Fe(III), 57Co(II), 64Cu(II) and 153Gd(III) were prepared with EDTA and its derivative containing the lipophilic 1-(4-methylphenyl)-group (MPEDTA), together with the corresponding 99mTc-compounds. The formation of these complexes was verified by electrophoresis and they were screened for potential use as MRI hepatobiliary contrast agents by biodistribution studies in mice. In this series, the MPEDTA complexes of 54Mn(II) and 64Cu(II) showed increased urinary excretion compared to the unsubstituted EDTA complexes, while the MPEDTA complexes of 99mTc, 59Fe, 57Co, 153Gd and particularly 51Cr demonstrated improved hepatobiliary excretion. Further lipophilic substitution should enhance this property but the preparation of such ligands is complicated by cyclisation reactions.