Synthesis and Evaluation of a Bifunctional Chelator for Thorium-227 Targeted Radiotherapy.

Thorium-227 (Th) is an α-emitting radionuclide currently under investigation for targeted alpha therapy. Available chelators used for this isotope suffer from challenging multistep syntheses. Here, we present the synthesis and preclinical evaluation of a novel bifunctional chelator, SCN-Bn-DOTHOPO, which contains an isothiocyanate group that is suitable for conjugation to biological molecules.

In Vivo Trafficking of the Anticancer Drug Tris(8-Quinolinolato) Gallium (III) (KP46) by Gallium-68/67 PET/SPECT Imaging.

KP46 (tris(hydroxyquinolinato)gallium(III)) is an experimental, orally administered anticancer drug. Its absorption, delivery to tumours, and mode of action are poorly understood. We aimed to gain insight into these issues using gallium-67 and gallium-68 as radiotracers with SPECT and PET imaging in mice.

Probing Unexpected Reactivity in Radiometal Chemistry: Indium-111-Mediated Hydrolysis of Hybrid Cyclen-Hydroxypyridinone Ligands.

Chelators based on hydroxypyridinones have utility in incorporating radioactive metal ions into diagnostic and therapeutic agents used in nuclear medicine. Over the course of our hydroxypyridinone studies, we have prepared two novel chelators, consisting of a cyclen (1,4,7,10-tetraazacyclododecane) ring bearing two pendant hydroxypyridinone groups, appended via methylene acetamide motifs at either the 1,4-positions () or 1,7-positions () of the cyclen ring. In radiolabeling reactions of or with the γ-emitting radioisotope, [In]In, we have observed radiometal-mediated hydrolysis of a single amide group of either or .

Toward Bifunctional Chelators for Thallium-201 for Use in Nuclear Medicine.

Auger electron therapy exploits the cytotoxicity of low-energy electrons emitted during radioactive decay that travel very short distances (typically <1 μm). Tl, with a half-life of 73 h, emits ∼37 Auger and other secondary electrons per decay and can be tracked as its gamma emissions enable SPECT imaging. Despite the useful nuclear properties of Tl, satisfactory bifunctional chelators to incorporate it into bioconjugates for molecular targeting have not been developed.

Non-invasive radionuclide imaging of trace metal trafficking in health and disease: "PET metallomics".

Several specific metallic elements must be present in the human body to maintain health and function. Maintaining the correct quantity (from trace to bulk) and location at the cell and tissue level is essential. The study of the biological role of metals has become known as metallomics.

To chelate thallium(I) - synthesis and evaluation of Kryptofix-based chelators for Tl.

While best known for its toxic properties, thallium has also been explored for applications in nuclear diagnostics and medicine. Indeed, [Tl]TlCl has been used extensively for nuclear imaging in the past before it was superceded by other radionuclides such as Tc. One reason for this loss of interest is the severe lack of suitable organic chelators able to effectively coordinate ionic forms of Tl and deliver it to specific diseased tissue by means of attached biological vectors.

Protocols for Dual Tracer PET/SPECT Preclinical Imaging.

Background: Multi-tracer PET/SPECT imaging enables different modality tracers to be present simultaneously, allowing multiple physiological processes to be imaged in the same subject, within a short time-frame. Fluorine-18 and technetium-99m, two commonly used PET and SPECT radionuclides, respectively, possess different emission profiles, offering the potential for imaging one in the presence of the other. However, the impact of the presence of each radionuclide on scanning the other could be significant and lead to confounding results.

Targeted Auger electron-emitter therapy: Radiochemical approaches for thallium-201 radiopharmaceuticals.

Introduction: Thallium-201 is a radionuclide that has previously been used clinically for myocardial perfusion scintigraphy. Although in this role it has now been largely replaced by technetium-99 m radiopharmaceuticals, thallium-201 remains attractive in the context of molecular radionuclide therapy for cancer micrometastases or single circulating tumour cells. This is due to its Auger electron (AE) emissions, which are amongst the highest in total energy and number per decay for AE-emitters.

Preparing for an Australian Football League Women's League Season.

The aims were to investigate the externally measured weekly loads, and the distribution intensity relative to the 1-min maximal mean (MM) intensity of matches. Athletes ( = 28) wore 10 Hz GNSS devices during training and matches. For the descriptive analysis, a range of movement variables were collected, including total distance, high-speed distance, very high-speed distance, acceleration, and acceleration load.

Quantifying the Movement Characteristics of Australian Football League Women's Competition.

Thornton, HR, Armstrong, CR, Gamble, T, Rigby, A, Johnston, RD, and Duthie, GM. Quantifying the movement characteristics of Australian Football League Women's competition. J Strength Cond Res 36(12): 3415-3421, 2022-The purpose is to provide an overview of the externally measured movement characteristics of Australian Football League Women's (AFLW) competition, and the variability in this between matches.

Greater Association of Relative Thresholds Than Absolute Thresholds With Noncontact Lower-Body Injury in Professional Australian Rules Footballers: Implications for Sprint Monitoring.

Unlabelled: Sprint capacity is an important attribute for team-sport athletes, yet the most appropriate method to analyze it is unclear.

Purpose: To examine the relationship between sprint workloads using relative versus absolute thresholds and lower-body soft-tissue and bone-stress injury incidence in professional Australian rules football.

Methods: Fifty-three professional Australian rules football athletes' noncontact soft-tissue and bone-stress lower-body injuries (N = 62) were recorded, and sprint workloads were quantified over ∼18 months using the global positioning system.