Automated radiolabeling and handling of 177Lu ‐ and 225Ac‐PSMA‐617 using a robotic pipettor
A commercially available robotic pipettor is used to perform automated radiolabeling of metal isotopes and processing of final product for quality control. The protocol and setup can easily be customized for each experiment and allows for minimum manual handling by and reduced exposure to the radiochemist. While automated modules for F-18 and C-11 radiosyntheses are standardized with features such as multiple reactors, vacuum connection and semi-preparative HPLC, labeling and processing of compounds with radiometals such as Zr-89, Lu-177 and Ac-225 often do not require complex manipulations and are frequently performed man...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 1, 2024 Category: Biochemistry Authors: Shin Hye Ahn, Anthony P. Belanger Tags: PROTOCOL Source Type: research

18F ‐Fluorination of a supported 2‐(aryl‐di‐tert‐butylsilyl)‐N‐methyl‐imidazole for indirect 18F‐labeling of a VHH single‐variable domain
Using a heterogeneous precursor, a18F-2-aryl-di-tert-butylfluorosilane possessing a pendant azido group was synthesized and bioconjugated to a VHH single-variable domain by strain-promoted alkyne –azide cycloaddition. Anchoring an imidazole-di-tert-butyl-arylsilane possessing an azido group to a polystyrene resin provided a heterogeneous precursor that was radiolabeled easily using aqueous [18F]fluoride. After optimizing the conditions (i.e., using DMSO as solvent and heating at 160 °C for 15 min), the desired [18F]fluorosilane was obtained in 24% radiochemical yield (RCY) and 78% radiochemical purity (RCP) using soli...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 16, 2024 Category: Biochemistry Authors: Marine Steffann, Guillaume Bluet, S ébastien Roy, Catherine Aubert, Eric Fouquet, Philippe Hermange Tags: RESEARCH ARTICLE Source Type: research

Synthesis of [3H]Org24598 using in ‐house prepared [3H]MeI
The synthesis of tritium-labelled glycine transporter 1 inhibitor Org24598 is reported. Because of the instability of the Org24598 skeleton under hydrogenation conditions, a five-step synthetic sequence using an in-house prepared tritium-labelled alkylating agent ([3H]MeI, SA  = 26.2 Ci/mmol) was employed. The synthesis of tritium-labelled glycine transporter 1 inhibitor Org24598 is reported. Because of the instability of the Org24598 skeleton under hydrogenation conditions, a synthetic approach using an in-house prepared tritium-labelled alkylating agent ([3H]MeI, SA  = 26.2 Ci/mmol) was employed. Alternative ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 15, 2024 Category: Biochemistry Authors: Michal Kriegelstein, Gabriela Nov áková, Aleš Marek Tags: RESEARCH ARTICLE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 15, 2024 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Preparation of [1 ′‐13C]citric acid as a probe in a breath test to evaluate tricarboxylic acid cycle flux
[1 ′-13C]Citric acid (1) was efficiently prepared from dimethyl 1,3-acetonedicarboxylate in two steps as a probe for a breath test. Compound1 was orally administrated to rats, and the measurements of the13CO2/12CO2 ratios in their breath were successfully performed. [1 ′-13C]Citric acid (1) was efficiently prepared from dimethyl 1,3-acetonedicarboxylate in two steps as a probe for a breath test. The synthetic method was selected because of the yield and reproducibility. Compound1 was orally administrated to rats, and the time course of the increase of13CO2/12CO2 ratios (Δ13CO2) in their breath was successfully followe...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 4, 2024 Category: Biochemistry Authors: Hidemichi Mitome, Mieko Takenishi, Kumiko Ono, Naoyuki Kawagoe, Tsunehiko Imai, Yosuke Sasaki, Yoshihisa Urita, Kazuki Akira Tags: RESEARCH ARTICLE Source Type: research

A facile synthesis of precursor for the σ‐1 receptor PET radioligand [18F]FTC‐146 and its radiofluorination
A one-step preparation of alkyl-chloride-based precursor AM-16 and its fluorination for the production of σ-1 receptor tracer [18F]FTC-146 was developed being the first successful instance of using an aliphatic chloride for 18F-fluorination, while not being mediated by intramolecular catalysis, and without requiring huge excess of the substrate.18F-fluorination of AM-16 led to a moderate decay-corrected radiochemical yield (RCY = 7.5%) with molar activity of 45.9 GBq/ μmol. A preliminary autoradiographic study of [18F]FTC-146 binding to σ-1 receptors in cryostat brain sections from an ArcSwe Alzheimer's disease model mo...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 4, 2024 Category: Biochemistry Authors: Anna Mare šová, Michal Jurášek, Pavel B. Drašar, Bohumil Dolenský, Elena A. Prokudina, Vladimir Shalgunov, Matthias M. Herth, Paul Cumming, Alexander Popkov Tags: RESEARCH ARTICLE Source Type: research

Open ‐source flow setup for rapid and efficient [18F]fluoride drying for automation of PET tracer syntheses
Unnecessary manual interventions increase the radiation exposure of personnel while compromising the reliability of syntheses. We have designed and evaluated a fully automated system for rapidly and effectively processing and drying aqueous [18F]fluoride that can be directly connected to the cyclotron. In addition, we present the beneficial usage of new developed automated flow processes to produce [18F]fluoroethyl tosylate (FEOTs) and [18F]fluoroethyl triflate (FEOTf), important ligands for late-stage fluoroethylation of PET tracers. One of the key strategies for radiochemical research facilities is the automation of synt...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 29, 2023 Category: Biochemistry Authors: Florian Menzel, Jonathan Cotton, Thomas Ziegler, Andreas Maurer, Jochen M. Neumaier Tags: RESEARCH ARTICLE Source Type: research

Development of radiotracers for riboflavin transporter 3 imaging in diseases —A brief overview
RFVT3 is a potential biomarker for use in the diagnosis and therapy of RFVT3-overexpressed diseases, such as oncologic and neurodegenerative diseases. Riboflavin (RF, vitamin B2) plays a key role in metabolic oxidation –reduction reactions, especially in the mitochondrial reprogramming of energy metabolism. Riboflavin transporter 3 (RFVT3) is a vital section of the mitochondrial network and involved in riboflavin homeostasis and production of adenosine triphosphate (ATP). The abnormal expression of RFVT3 is clos ely associated with the occurrence and progression of multiple diseases. Therefore, it is vital to understand ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 23, 2023 Category: Biochemistry Authors: Jindian Li, Xianzhong Zhang Tags: PERSPECTIVE Source Type: research

Validation of a good manufacturing practice procedure for the production of [11C]AZD4747, a CNS penetrant KRASG12c inhibitor
A GMP-compliant production of [11C]AZD4747 was developed to enable PET studies in human subjects. Graphical abstract was created usingBiorender.com. AZD4747 is a KRASG12C inhibitor recently shown to cross the non-human primate blood-brain barrier efficiently. In the current study, a GMP-compliant production of [11C]AZD4747 was developed to enable PET studies in human subjects. The validated procedure afforded [11C]AZD4747 as an injectable solution in good radioactivity yield (1656  ± 532 MBq), excellent radiochemical purity (100%), and a molar activity of 77 ± 13 GBq/μmol at the end of the synthesis, which t...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 21, 2023 Category: Biochemistry Authors: Miguel A. Cort és González, Antonia A. Högnäsbacka, Christer Halldin, Magnus Schou Tags: PROTOCOL Source Type: research

Automated radiosynthesis of [18F]CETO, a PET radiotracer for imaging adrenal glands, on Synthra RNplus
In this paper, we show how we were able to produce [18F]CETO, an important adrenal gland imaging agent, on a Synthra RNplus instrument. This paper includes the synthesis instructions, quality control and validation procedures, which were completed for routine GMP clinical productions of this radiotracer to occur. Primary aldosteronism (PA) is the leading secondary cause of hypertension. Determining whether one (unilateral) or both (bilateral) adrenal glands are the source of PA in a patient remains challenging, and yet it is a critical step in the decision whether to recommend potentially curative surgery (adrenalectomy) o...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 20, 2023 Category: Biochemistry Authors: Matthew Hird, Joseph J. Russell, Lei Li Corrigan, Istvan Boros, Patrik Nordeman, Gunnar Antoni, Mark Gurnell, Franklin I. Aigbirhio Tags: PROTOCOL Source Type: research