A novel annexin A5 derivative (cys-annexin A5) with a single cysteine residue at its C-terminal has been developed and successfully labeled in high labeling yield with (99m)Tc by a ligand exchange reaction. Like the 1st generation (99m)Tc-HYNIC-annexin A5, the novel (99m)Tc-cys-annexin A5 derivative shows in normal mice mainly renal and, to a lesser extent, hepatobiliary excretion. In rat model...

A murine, apoptosis-inducing monoclonal antibody (mTRA-8) targeting human DR5 was radiolabeled with Tc-99m. The binding affinity (K(d)) and the number of DR5 receptors were measured in MD MBA-231-derived 2LMP cell lines that were "sensitive" or "resistant" to mTRA-8 killing. Single-photon emission computed tomography and X-ray computed tomography (SPECT/CT) evaluated the Tc-99m-mTRA-8 retention...

Two propylene amine oxime (PnAO) complexes, 1, containing a 3-nitro-1,2,4-triazole and 2, containing two 3-nitro-1,2,4-triazoles, were synthesized and radiolabeled with (99m)Tc in high labeling yields. Cellular uptakes of (99m)Tc-1 and (99m)Tc-2 were tested using a S180 cells line. Under anoxic conditions, the cellular uptakes of (99m)Tc-1 and (99m)Tc-2 were 33.7 ± 0.2% and 35.0 ± 0.7% at 4 h, ...

A simple and efficient method for radiolabeling preformed liposomes was developed using hepatobiliary imaging agent (99m)Tc-diisopropyl iminodiacetic acid ((99m)Tc-DISIDA). Chloroform extraction of (99m)Tc-DISIDA from aqueous solutions results in 80% radioactivity in the organic phase due to its lipophilic properties. However, with the presence of reduced glutathione (gamma-Glu-Cys-Gly), chloro...

UNLABELLED Prostate-specific membrane antigen (PSMA) is highly expressed in prostate cancer, and small-molecule radiopharmaceuticals targeting PSMA rapidly detect the location and extent of disease. Here we evaluated preclinically 4 novel (99m)Tc-labeled small-molecule inhibitors of PSMA with the potential for clinical translation for molecular imaging of prostate cancer in humans. METHODS Fo...

AIM Various studies have been conducted for determining the most optimal method for the early diagnosis of local recurrent or distant metastatic thyroid cancers. The aim of this study was to evaluate the clinical utility of technetium-99m (Tc-99m)-labeled octreotide derivatives in the detection of recurrence or distant metastases in medullary thyroid cancer patients and to compare the lesions w...

Radiopharmaceuticals are known to interact with the blood components (i.e. the red blood cells, serum proteins etc) but so far, there have been no data regarding their purely mechanical trapping in thrombi. The experiments presented in this communication provide evidence that the technetium-99m labeled albumin macroaggregate ((99m)Tc-MAA), apparently due to its particle size, can be almost quan...

Tannic acid is a polyphenolic compound that could be labeled with technetium-99m. To produce about 90% yield of  (99m)Tc-tannic acid in acidic media (pH), the conditions required were 150 μg tin chloride, 30 min reaction time, and 200 μg of the substrate. (99m)Tc-tannic was stable for 6 h. Oral biodistribution of (99m)Tc-tannic showed that it concentrated in the stomach ulcer to reach about 50%...

BACKGROUND The receptor for advanced glycation end products (RAGE) is implicated in the development and progression of atherosclerosis. We tested the hypothesis that (99m)Tc-labeled anti-RAGE F(ab')(2) can be used as a noninvasive tool to image atherosclerotic lesions in apolipoprotein E-deficient (apoE(-/-)) mice. METHODS AND RESULTS A sequence in the V-type Ig extracellular domain of RAGE w...

UNLABELLED It was previously shown that the (99m)Tc-labeled hydrazinonicotinamide (HYNIC)-conjugated LTB4 antagonist MB81 visualized infectious foci in rabbits adequately and within a few hours after injection. Here, the bivalent HYNIC-conjugated LTB4 antagonist MB67 (analog of MB81) was fluorinated with (18)F via hydrazone formation and tested in vivo. METHODS MB67 was [(18)F]-fluorinated vi...