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Journals Journal of Labelled Compounds ...

Journal of Labelled Compounds & Radiopharmaceuticals

https://read.qxmd.com/read/38485465/preparation-characterization-and-radiolabeling-of-anti-her2-scfv-with-technetium-tricarbonyl-and-stability-studies
#1
JOURNAL ARTICLE
Negar Bozorgchami, Maryam Ahmadzadeh, Dara Hatamabadi, Abdolreza Yazdani, Soraya Shahhosseini, Elham Mohit
Breast 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. HER2-targeted imaging via an appropriate radionuclide is a promising method for sensitive and accurate identification of HER2+ primary and metastatic lesions. 99m Tc-anti-HER2 scFv can specifically target malignancies and be used for diagnosis of the cancer type and metastasis as well as treatment of breast cancer...
March 14, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38442415/synthesis-of-stable-isotope-tritiated-and-carbon-14-labeled-balcinrenone
#2
JOURNAL ARTICLE
Jonas Bergare, Christopher Bailey, Henrik Sörensen, Gunnar Grönberg, Karl Broberg, Monica Berglund, Tudor Grecu, Carolina Sanchez, Hans Emtenäs, Ryan A Bragg, Charles S Elmore
As 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...
March 5, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38369901/automated-radiosynthesis-of-mglur5-pet-tracer-18-f-fpeb-from-aryl-chloro-precursor-and-validation-for-clinical-application
#3
JOURNAL ARTICLE
Mahabuba Jahan, Arsalan Amir, Arindam Das, Jacob Kihlström, Sangram Nag
The radioligand [18 F]FPEB, used for PET imaging of the brain's metabotropic glutamate receptor subtype 5 (mGluR5), undergoes a thorough validation process to ensure its safety, efficacy, and quality for clinical use. The process starts by optimizing the synthesis of [18 F]FPEB to achieve high radiochemical yield and purity. This study focuses on optimizing the radiolabeling process using an aryl-chloro precursor and validating the GMP production for clinical applications. Fully automated radiolabeling was achieved via one-step nucleophilic substitution reaction...
February 19, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38342496/formulation-of-patient-dose-of-177-lu-lu-trastuzumab-using-in-house-developed-freeze-dried-kit-a-path-forward-for-clinical-translation
#4
JOURNAL ARTICLE
Jeyachitra Amirdhanayagam, Mohini Guleria, Rohit Sharma, Naveen Kumar, Archana Mukherjee, Tapas Das
Trastuzumab is a US-FDA-approved humanized monoclonal antibody used for the treatment of human epidermal growth factor receptor 2 (HER2)-positive breast cancer. The aim of the present work is to optimize a freeze-dried formulation of DOTA-Trastuzumab conjugate for the preparation of patient doses of [177 Lu]Lu-Trastuzumab for radioimmunotherapy of breast cancer. The formulation of [177 Lu]Lu-Trastuzumab usually takes a long time, and thus, such a process is not suitable for the routine preparation of this agent in hospital radiopharmacies...
February 11, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38332677/tritium-and-deuterium-labelling-of-a-kainate-receptor-antagonist-and-evaluation-as-a-radioligand
#5
JOURNAL ARTICLE
Paulina Chałupnik, Aleš Marek, Marie Emilie Leiticia Hovah, Darryl S Pickering, Piero Temperini, Stephanie Donbosco, Ewa Szymańska, Tommy N Johansen
Kainate receptors play a crucial role in mediating synaptic transmission within the central nervous system. However, the lack of selective pharmacological tool compounds for the GluK3 subunit represents a significant challenge in studying these receptors. Recently presented compound 1 stands out as a potent antagonist of GluK3 receptors, exhibiting nanomolar affinity at GluK3 receptors and strongly inhibiting glutamate-induced currents at homomeric GluK1 and GluK3 receptors in HEK293 cells with Kb values of 65 and 39 nM, respectively...
February 8, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38296817/automated-radiolabeling-and-handling-of-177-lu-and-225-ac-psma-617-using-a-robotic-pipettor
#6
JOURNAL ARTICLE
Shin Hye Ahn, Anthony P Belanger
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 manually by a radiochemist. These procedures typically involve transferring solutions to and from vials using pipettes followed by heating of the reaction mixture, and do not require all the features found in most commercial automated synthesis units marketed as F-18 or C-11 modules...
January 31, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38224624/-18-f-fluorination-of-a-supported-2-aryl-di-tert-butylsilyl-n-methyl-imidazole-for-indirect-18-f-labeling-of-a-v-h-h-single-variable-domain
#7
JOURNAL ARTICLE
Marine Steffann, Guillaume Bluet, Sébastien Roy, Catherine Aubert, Eric Fouquet, Philippe Hermange
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 [18 F]fluoride. After optimizing the conditions (i.e., using DMSO as solvent and heating at 160°C for 15 min), the desired [18 F]fluorosilane was obtained in 24% radiochemical yield (RCY) and 78% radiochemical purity (RCP) using solid-phase extraction as sole purification. Then, this compound was conjugated by strain-promoted alkyne-azide cycloaddition to a model single-variable domain possessing a cyclooctyne tag, yielding to the desired 18 F-labeled bioconjugate in 2% RCY and >95% RCP after purification by a size exclusion chromatography...
January 15, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38221662/synthesis-of-3-h-org24598-using-in-house-prepared-3-h-mei
#8
JOURNAL ARTICLE
Michal Kriegelstein, Gabriela Nováková, Aleš Marek
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 ([3 H]MeI, SA = 26.2 Ci/mmol) was employed. Alternative methods of labelling are discussed.
January 14, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38171549/preparation-of-1-13-c-citric-acid-as-a-probe-in-a-breath-test-to-evaluate-tricarboxylic-acid-cycle-flux
#9
JOURNAL ARTICLE
Hidemichi Mitome, Mieko Takenishi, Kumiko Ono, Naoyuki Kawagoe, Tsunehiko Imai, Yosuke Sasaki, Yoshihisa Urita, Kazuki Akira
[1'-13 C]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. Compound 1 was orally administrated to rats, and the time course of the increase of 13 CO2 /12 CO2 ratios (Δ13 CO2 ) in their breath was successfully followed, indicating the metabolism of 1. Thus, the 13 C-breath test using 1 is a promising method to evaluate tricarboxylic acid (TCA) cycle flux.
January 3, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38171540/a-facile-synthesis-of-precursor-for-the-%C3%AF-1-receptor-pet-radioligand-18-f-ftc-146-and-its-radiofluorination
#10
JOURNAL ARTICLE
Anna Marešová, Michal Jurášek, Pavel B Drašar, Bohumil Dolenský, Elena A Prokudina, Vladimir Shalgunov, Matthias M Herth, Paul Cumming, Alexander Popkov
The σ-1 receptor is a non-opioid transmembrane protein involved in various human pathologies including neurodegenerative diseases, inflammation, and cancer. The previously published ligand [18 F]FTC-146 is among the most promising tools for σ-1 molecular imaging by positron emission tomography (PET), with a potential for application in clinical diagnostics and research. However, the published six- or four-step synthesis of the tosyl ester precursor for its radiosynthesis is complicated and time-consuming...
January 3, 2024: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38155110/open-source-flow-setup-for-rapid-and-efficient-18-f-fluoride-drying-for-automation-of-pet-tracer-syntheses
#11
JOURNAL ARTICLE
Florian Menzel, Jonathan Cotton, Thomas Ziegler, Andreas Maurer, Jochen M Neumaier
One of the key strategies for radiochemical research facilities is the automation of synthesis processes. Unnecessary manual operations increase the radiation exposure of personnel, while simultaneously threatening the reliability of syntheses. We have previously reported an affordable open-source system comprising 3D-printed continuous flow reactors, a custom syringe pump, and a pressure regulator that can be used to perform radiofluorinations. In this paper, we address additional essential processes that are needed for radiotracer development and synthesis, with the aim of making laboratory work safer and research more efficient...
December 28, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38131157/development-of-radiotracers-for-riboflavin-transporter-3-imaging-in-diseases-a-brief-overview
#12
JOURNAL ARTICLE
Jindian Li, Xianzhong Zhang
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 closely associated with the occurrence and progression of multiple diseases. Therefore, it is vital to understand the riboflavin internalization pathway under pathological conditions by addressing the abnormal expression of RFVT3, which could be a highly valuable biomarker for the early diagnosis and effective therapy of various diseases...
December 22, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38124264/validation-of-a-good-manufacturing-practice-procedure-for-the-production-of-11-c-azd4747-a-cns-penetrant-kras-g12c-inhibitor
#13
JOURNAL ARTICLE
Miguel A Cortés González, Antonia A Högnäsbacka, Christer Halldin, Magnus Schou
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 [11 C]AZD4747 was developed to enable PET studies in human subjects. The validated procedure afforded [11 C]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 took 46 ± 1 min from the end of the bombardment...
December 20, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38116667/automated-radiosynthesis-of-18-f-ceto-a-pet-radiotracer-for-imaging-adrenal-glands-on-synthra-rnplus
#14
JOURNAL ARTICLE
Matthew Hird, Joseph J Russell, Lei Li Corrigan, Istvan Boros, Patrik Nordeman, Gunnar Antoni, Mark Gurnell, Franklin I Aigbirhio
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) or lifelong medical therapy (typically requiring multiple drugs). Recently, we have developed a fluorine-18 radiopharmaceutical [18 F]CETO to permit greater access to PA molecular imaging. Herein, we report an automated synthesis of this radiotracer...
December 20, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38073118/-11c-co2-bop-fixation-with-amines-to-access-11c-labeled-ureas-for-pet-imaging
#15
JOURNAL ARTICLE
Coralie M Bonnemaire, Albert D Windhorst, Romano Orru, Eelco Ruijter, Danielle J Vugts
Carbon-11 (11 C) is a widely used radionuclide for positron emission tomography (PET) owing to the omnipresence of carbon atoms in organic molecules. While its half-life of 20.4 min is ideal for imaging and dosimetry, it also limits the synthetic possibilities. As such, the development of fast and easy, high-yielding synthesis methods is crucial for the application of 11 C-labeled tracers in humans. In this study, we present a novel and efficient method for the reaction of [11 C]CO2 with amine precursors using benzotriazole-1-yl-oxy-tris-(dimethylamino)-phosphonium hexafluorophosphate (BOP) to access 11 C-labeled ureas...
December 10, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38066721/-14-c-radiolabeling-of-a-new-steroidal-antiandrogen-with-a-c-18-angular-methyl-extension
#16
JOURNAL ARTICLE
Jean-Yves Sancéau
The synthesis of a 14 C-labeled C-18 functionalized steroid (as referred as EM-6798) that will serve as a probe for the research of novel antiandrogens has been accomplished. This radioactive steroid was obtained in nine steps by coupling racemic N-cyclohexyl-1-(3'-hydroxy[U-14 C]phenyl)propylamine with protected 18-bromomethyl-3,17-androstenedione. Incorporation of the radiolabel on the C-18 side chain was achieved using commercially available 3-bromo[U-14 C]phenol. Alkylation of N-cyclohexyl-1-(3'-hydroxy[U-14 C]phenyl)propylamine with 3-ethylenedioxy-18-bromomethyl-3,17-androstenedione furnished after reduction and deprotection, [phenyl-U-14 C]EM-6798 in a 20% overall yield from 3-bromo[U-14 C]phenol at a specific activity of 156 μCi/mg with 97...
December 8, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/38044291/synthesis-and-spectroscopic-characterization-of-13-c-4-labeled-4-cyano-2-oxobutyraldehyde-semicarbazone-a-metabolite-of-nitrofurazone
#17
JOURNAL ARTICLE
Anuradha Singh, David J Smith, Gary D Strahan, Steven J Lehotay
Nitrofurazone usage in food-producing animals is prohibited in most countries, including the United States. Regulatory agencies regularly monitor its use in domestic, export/import animals' food products by measuring the semicarbazide (SEM) metabolite as a biomarker of nitrofurazone exposure. However, the use of SEM is controversial because it is also produced in food naturally and thus gives false positive results. A cyano-metabolite, 4-cyano-2-oxobutyraldehyde semicarbazone (COBS), is proposed as an alternate specific marker of nitrofurazone to distinguish nitrofurazone from treated or untreated animals...
December 3, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/37985145/synthesis-of-trifold-labeled-versatile-reagent-3-5-13-c-2-4-15-%C3%A2-n-4-phenyl-1-2-4-triazoline-3-5-dione
#18
JOURNAL ARTICLE
Frederic Bourgeois, Ulrich Höller, Thomas Netscher
Triazolinediones are an important class of derivatization agents that have found application in various research disciplines. Their unique reactivity often allows precise and selective tagging of relevant molecular scaffolds to facilitate structural elucidation, tracking in biological systems, and stabilization of labile compounds. Recent research efforts mainly focused on the development of novel fluorescent and ionizable or isotopically labeled tags improving the quantification and identification of the parent molecule by suitable analytical methods...
November 20, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/37957035/novel-synthesis-of-11-c-labeled-imidazolines-via-pd-0-mediated-11-c-carbomethoxylation-using-11-c-co-and-arylborons
#19
JOURNAL ARTICLE
Hideki Ishii, Katsuyuki Minegishi, Kotaro Nagatsu, Nobuki Nengaki, Ming-Rong Zhang
A labeling technique was developed for the imidazoline I2 receptor ligand 2-(3-fluoro-tolyl)-4, 5-dihydro-1H-imidazole (FTIMD) using Pd(0)-mediated 11 C-carbomethoxylation with [11 C]CO, followed by imidazoline ring formation with ethylenediamine-trimethylaluminium (EDA-AlMe3 ). To achieve this, [11 C]CO was passed through a methanol (MeOH) solution containing 3-fluoro-4-methylphenylboronic acid (1), palladium (II) acetate (Pd [OAc]2 ), triphenylphosphine (PPh3 ), and p-benzoquinone (PBQ). The mixture was then heated at 65°C for 5 min...
November 13, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/37941144/facile-synthesis-of-14-c-nitrofurazone-from-14-c-urea
#20
JOURNAL ARTICLE
Anuradha Singh, David J Smith
The veterinary drug nitrofurazone (5-nitro-2-furaldehyde semicarbazone) exhibits excellent antimicrobial properties but its application in food-producing animals is prohibited. The illegal use of nitrofurazone is regularly monitored by food regulatory agencies. Currently, semicarbazide (SEM) is used as a marker of nitrofurazone exposure. However, the use of SEM as a marker of nitrofurazone is under scrutiny after evidence of a high incidence of false positive tests. To overcome the current dilemma, it is necessary to identify a nitrofurazone-specific marker analyte which requires conducting nitrofurazone metabolism studies in food-producing animals...
November 8, 2023: Journal of Labelled Compounds & Radiopharmaceuticals
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