Preparation, Characterization, and Radiolabeling of Anti ‐HER2 scFv With Technetium Tricarbonyl and Stability Studies
Radiolabeling of anti-HER2 scFv derived from trastuzumab with technetium-99m by in-house prepared99mTc-tricarbonyl resulted in99mTc-anti-HER2 scFv with radiochemical purity of around 98% and with no change in biological activity.99mTc-anti-HER2 scFv was stable for at least 24  h in PBS buffer, normal saline, human plasma proteins, and histidine solution. ABSTRACTBreast cancer is the most common diagnosed cancer, and the second cause of cancer death among women, worldwide. HER2 overexpression occurred in approximately 15% to 20% of breast cancers. Invasive biopsy method has been used for detection of HER2 overexpression. ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 15, 2024 Category: Biochemistry Authors: Negar Bozorgchami, Maryam Ahmadzadeh, Dara Hatamabadi, Abdolreza Yazdani, Soraya Shahhosseini, Elham Mohit Tags: RESEARCH ARTICLE Source Type: research

Synthesis of Stable Isotope, Tritiated, and Carbon ‐14 Labeled Balcinrenone
ABSTRACTAs part of a medicinal chemistry program aimed at discovering a mineralocorticoid receptor modulator for treatment of kidney and cardiovascular indications, multiple labeled versions of the lead compound, balcinrenone (AZD9977), were prepared. Four stable isotope labeled versions of the compound were prepared for clinical bioanalysis and biological investigations. Three of these stable isotope labeled compounds were tritiated as well as the parent for biology applications and DMPK investigations. They were prepared using a standard iodination –tritiodehalogentation approach. Finally, AZD9977 was prepared in carbo...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 6, 2024 Category: Biochemistry Authors: Jonas Bergare, Christopher Bailey, Henrik S örensen, Gunnar Grönberg, Karl Broberg, Monica Berglund, Tudor Grecu, Carolina Sanchez, Hans Emtenäs, Ryan A. Bragg, Charles S. Elmore 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 - March 4, 2024 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Automated radiosynthesis of mGluR5 PET tracer [18F]FPEB from aryl ‐chloro precursor and validation for clinical application
In conclusion, the validation of [18F]FPEB involved a comprehensive process of synthesis optimization, quality control, which ensure the safety, efficacy, and quality of [18F]FPEB, enabling its reliable use in clinical PET. Here, we successfully radiolabeled and validated [18F]FPEB using aryl-chloro precursor according to GMP production for clinical application. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 29, 2024 Category: Biochemistry Authors: Mahabuba Jahan, Arsalan Amir, Arindam Das, Jacob Kihlstr öm, Sangram Nag Tags: PROTOCOL 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 - February 12, 2024 Category: Biochemistry Authors: Jindian Li, Xianzhong Zhang Tags: PERSPECTIVE 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 - February 12, 2024 Category: Biochemistry Tags: ISSUE INFORMATION 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 - February 12, 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 - February 12, 2024 Category: Biochemistry Authors: Florian Menzel, Jonathan Cotton, Thomas Ziegler, Andreas Maurer, Jochen M. Neumaier Tags: RESEARCH ARTICLE 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 - February 12, 2024 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

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 12, 2024 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Formulation of patient dose of [177Lu]Lu ‐Trastuzumab using in‐house developed freeze‐dried kit: A path forward for clinical translation
Trastuzumab is a US-FDA approved humanized monoclonal antibody used for immunotherapy of human epidermal growth factor receptor 2 (HER2) positive breast cancer. Radioimmunotherapy of ca breast employing [177Lu]Lu-Trastuzumab is currently undergoing clinical investigations. In the present work, formulation of patient dose of [177Lu]Lu-Trastuzumab using an in-house developed freeze-dried kit of DOTA-Trastuzumab has been demonstrated. The efficacy of [177Lu]Lu-Trastuzumab towards targeting HER2 receptors was showcased by detailed in vitro and ex vivo studies in cancer cell lines and small animal model, respectively. Trastuzum...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 12, 2024 Category: Biochemistry Authors: Jeyachitra Amirdhanayagam, Mohini Guleria, Rohit Sharma, Naveen Kumar, Archana Mukherjee, Tapas Das Tags: RESEARCH ARTICLE Source Type: research

Tritium and deuterium labelling of a kainate receptor antagonist and evaluation as a radioligand
This study presents the synthesis of two potent GluK3-preferring iodine derivatives of compound1, serving as precursors for radiolabelling. Furthermore, we demonstrate the optimisation of dehalogenation conditions using hydrogen and deuterium, resulting in [2H]-1, and demonstrate the efficient synthesis of the radioligand [3H]-1 with a specific activity of 1.48  TBq/mmol (40.1 Ci/mmol). Radioligand binding studies conducted with [3H]-1 as a radiotracer at GluK1, GluK2, and GluK3 receptors expressed in Sf9 and rat P2 membranes demonstrated its potential applicability for selectively studying native GluK3 receptors in the...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 9, 2024 Category: Biochemistry Authors: Paulina Cha łupnik, Aleš Marek, Marie Emilie Leiticia Hovah, Darryl S. Pickering, Piero Temperini, Stephanie Donbosco, Ewa Szymańska, Tommy N. Johansen Tags: RESEARCH ARTICLE Source Type: research