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Journal of Labelled Compounds & Radiopharmaceuticals

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https://www.readbyqxmd.com/read/29341227/pet-radiometals-for-antibody-labeling
#1
Eduardo Aluicio-Sarduy, Paul A Ellison, Todd E Barnhart, Weibo Cai, Robert Jerry Nickles, Jonathan W Engle
Recent advances in molecular characterization of tumors have made possible the emergence of new types of cancer therapies where the traditional cytotoxic drugs and nonspecific chemotherapy can be complemented with targeted molecular therapies. One of the main revolutionary treatments is the use of monoclonal antibodies (mAbs) that selectively target the disseminated tumor cells while sparing normal tissues. mAbs and related therapeutics can be efficiently radiolabeled with a wide range of radionuclides to facilitate preclinical and clinical studies...
January 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29341222/89-zr-immunopet-companion-diagnostics-and-their-impact-in-clinical-drug-development
#2
REVIEW
Brooke N McKnight, Nerissa T Viola-Villegas
Therapeutic monoclonal antibodies (mAbs) have been used in cancer treatment for 30 years, with around 24 mAb and mAb:drug conjugates approved by the FDA to date. Despite their specificity, efficacy has remained limited, which, in part, derails nascent initiatives towards precision medicine. An image-guided approach to reinforce treatment decisions using immune positron emission tomography (immunoPET) companion diagnostic is warranted. This review provides a general overview of current translational research using Zr-89 immunoPET and opportunities for utilizing and harnessing this tool to its full potential...
January 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29336065/optimization-of-18-f-syntheses-using-19-f-reagents-at-tracer-level-concentrations-and-lc-ms-ms-analysis-improved-synthesis-of-18-f-mdl100907
#3
Xiang Zhang, Ryan Dunlow, Burchelle N Blackman, Rolf E Swenson
Traditional radiosynthetic optimization faces the challenges of high radiation exposure, cost and inability to perform serial reactions due to tracer decay. To accelerate tracer development, we have developed a strategy to simulate radioactive 18 F-syntheses by using tracer-level (nanomolar) non-radioactive 19 F-reagents and LC-MS/MS analysis. The methodology was validated with fallypride synthesis under tracer-level 19 F-conditions, which showed reproducible and comparable results with radiosynthesis, and proved the feasibility of this process...
January 16, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29331022/open-letter-to-journal-editors-on-international-consensus-radiochemistry-nomenclature-guidelines
#4
Heinz H Coenen, Antony D Gee, Michael Adam, Gunnar Antoni, Cathy S Cutler, Yasuhisa Fujibayashi, Jae Min Jeong, Robert H Mach, Thomas L Mindt, Victor W Pike, Albert D Windhorst
No abstract text is available yet for this article.
January 13, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29323418/synthesis-of-2-d-acrylamide
#5
Alexey V Salin, Rashid Z Musin
2-d-Acrylamide was synthesized via the two-step procedure starting from acrylonitrile and deuterium oxide. This procedure affords 2-d-acrylamide in 99.9% chemical purity and 98.4% isotopic enrichment.
January 11, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29314233/heinz-h-coenen-a-pioneer-in-the-field-of-nuclear-and-radiochemistry
#6
Antony Gee, Bernd Neumaier
No abstract text is available yet for this article.
January 4, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29314210/heinz-h-coenen-a-great-radiopharmaceutical-chemist
#7
P August Schubiger
No abstract text is available yet for this article.
January 4, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29314165/synthesis-of-c-14-labeled-gabaa-%C3%AE-2-%C3%AE-3-selective-partial-agonists-and-the-investigation-of-late-occurring-and-long-circulating-metabolites-of-gabaa-receptor-modulator-azd7325
#8
Markus Artelsmair, Chungang Gu, Richard J Lewis, Charles S Elmore
Anxiolytic activity has been associated with GABAA α2 and α3 subunits. Several target compounds were identified and required in C-14 labeled form to enable a better understanding of their DMPK properties. AZD7325 is a selective GABAA α2 and α3 receptor modulator intended for the treatment of anxiety through oral administration. A great number of AZD7325 metabolites were observed across species in vivo, whose identification was aided by [14 C]AZD7325. An interesting metabolic cyclization and aromatization pathway leading to the tricyclic core of M9 and the oxidative pathways to M10 and M42 are presented...
January 4, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29314161/a-novel-synthesis-of-6-18-f-fluoromaltotriose-as-a-pet-tracer-for-imaging-bacterial-infection
#9
Mohammad Namavari, Gayatri Gowrishankar, Ananth Srinivasan, Sanjiv S Gambhir
The aim of this study was to develop a positron emission tomography (PET) tracer to visualize and monitor therapeutic response to bacterial infections. In our continued efforts to find maltose based PET tracers that can image bacterial infections, we have designed and prepared 6''-[18 F]fluoromaltotriose as a second generation PET imaging tracer targeting the maltodextrin transporter of bacteria. We have developed methods to synthesize 6''-deoxy-6''-[18 F]fluoro-α-D-glucopyranosyl-(1-4)-O-α-D-glucopyranosyl-(1-4)-O-D-glucopyranose (6''-[18 F]-fluoromaltotriose) as a bacterial infection PET imaging agent...
January 4, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29278650/synthesis-of-15-n-cholamine-bromide-hydrobromide
#10
Judy Szeto, Remy Lemoine, Rosary Nguyen, Lori L Olson, Mary J Tanga
[15 N]-Cholamine is an isotope tag for metabolomics research, because it possesses two important properties: an NMR active isotope and a permanent charge for MS sensitivity. Here we present a scalable synthesis of [15 N]-cholamine.
December 26, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29274290/facile-synthesis-of-high-specific-activity-4-1-14-c-butyl-1-2-diphenylpyrazolidine-3-5-dione-phenylbutazone-using-nucleophilic-substitution
#11
Anuradha Singh, Heldur Hakk, Sara J Lupton
Metabolism, environmental fate, and low concentration food residue studies would be facilitated by the use of radiolabeled test articles which can be readily quantified within complex matrices. However, radiochemical approaches for such studies require high specific activities to allow analytical detection of correspondingly low masses of test article. The synthesis of high specific activity (>50 μCi/μmol) [14 C] radiolabeled phenylbutazone presents a challenge using existing methodology, mainly due to the low solvent volumes required and vigorous refluxing needed to close the pyrazolidinedione ring...
December 23, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29274276/recent-progress-in-11-c-carbon-dioxide-11-c-co2-and-11-c-carbon-monoxide-11-c-co-chemistry
#12
Carlotta Taddei, Antony D Gee
[11 C]Carbon dioxide ([11 C]CO2 ) and [11 C]carbon monoxide ([11 C]CO) are two attractive precursors for labelling the carbonyl position (C=O) in a vast range of functionalised molecules (e.g. ureas, amides and carboxylic acids). The development of radiosynthetic methods to produce functionalised 11 C-labelled compounds is required to enhance the radiotracers available for positron emission tomography (PET), molecular and medical imaging applications. Following a brief summary of secondary 11 C-precursor production and uses, the review focuses on recent progress with direct 11 C-carboxylation routes with [11 C]CO2 and 11 C-carbonylation with [11 C]CO...
December 23, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29271003/evaluation-of-a-p-n-ligated-iridium-i-catalyst-in-hydrogen-isotope-exchange-reactions-of-aryl-and-heteroaryl-compounds
#13
Mégane Valero, Annina Burhop, Kristof Jess, Remo Weck, Matthias Tamm, Jens Atzrodt, Volker Derdau
We have developed a novel and efficient iridium-catalyzed hydrogen isotope exchange (HIE) reaction method with secondary and tertiary sulfonamides at ambient temperatures. Furthermore N-oxides and phosphonamides have been successfully applied in HIE reactions with moderate to excellent deuterium introduction.
December 21, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29247459/131-i-radiolabeled-immune-albumin-nanospheres-loaded-with-doxorubicin-for-in-vivo-combinatorial-therapy
#14
Anping Ji, Yuanchao Zhang, Gaochao Lv, Jianguo Lin, Ning Qi, Faquan Ji, Minghua Du
For the purpose of providing a new insights for high-efficiency radiochemotherapy of hepatoma, a radioimmunotherapy and chemotherapy combinatorial therapy albumin nanospheres 131 I-antiAFPMcAb-DOX-BSA-NPs was designed and prepared. It was obtained in a high radiolabeling yield (RLY) about 65% with the radiochemical purity (RCP) of over 98%. The transmission electron microscope (TEM) showed that the nanospheres obtained in good monodispersion with a diameter of approximately 230 nm. The doxorubicin (DOX) loading capacity of the DOX-BSA-NPs nanoparticles was determined to about 180 μg/mg and 95...
December 16, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29247455/synthesis-and-evaluation-of-an-18-f-labeled-trifluoroborate-derivative-of-2-nitroimidazole-for-imaging-tumor-hypoxia-with-positron-emission-tomography
#15
Paulo Sérgio Gonçalves Nunes, Zhengxing Zhang, Hsiou-Ting Kuo, Chengcheng Zhang, Julie Rousseau, Etienne Rousseau, Joseph Lau, Daniel Kwon, Ivone Carvalho, François Bénard, Kuo-Shyan Lin
2-Nitroimidazole-based hypoxia imaging tracers such as 18 F-FMISO are normally imaged at late time points (several hours post-injection) due to their slow clearance from background tissues. Here we investigated if a hydrophilic zwitterion-based ammoniomethyl-trifluoroborate derivative of 2-nitroimidazole, 18 F-AmBF3 -Bu-2NI, could have the potential to image tumor hypoxia at earlier time points. AmBF3 -Bu-2NI was prepared in four steps. 18 F labeling was conducted via 18 F-19 F isotope exchange reaction, and 18 F-AmBF3 -Bu-2NI was obtained in 14...
December 16, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29231250/synthesis-of-stable-isotope-labeled-nasturlexins-and-potential-precursors-to-probe-biosynthetic-pathways-of-cruciferous-phytoalexins
#16
M Soledade C Pedras, Q Huy To
The syntheses of perdeuterated phytoalexins nasturlexins A and C, and putative biosynthetic precursors, including phenylethyl isothiocyanates and phenylethyl dithiocarbamates, using commercially available [2,3,4,5,6-D5 ]phenylalanine, [2,3,4,5,6-D5 ]nitrobenzene and [2,3,4,5,6-D5 ]benzaldehyde are described. In addition, application of an efficient deuterium-hydrogen exchange transformation to non-labeled starting materials allowed access to new deuterated compounds, including 3-hydroxyphenylethyl glucosinolate...
December 12, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29231247/biocatalysis-in-radiochemistry-enzymatic-incorporation-of-pet-radionuclides-into-molecules-of-biomedical-interest
#17
REVIEW
Eunice S da Silva, Vanessa Gómez-Vallejo, Fernando López-Gallego, Jordi Llop
Biocatalysis is emerging as a new approach to radiolabel biologically active molecules with short half-lived positron emitters for their use in positron emission tomography. Despite the golden era of biocatalysis in radiochemistry occurred in the 70´s and 80´s, advances in enzyme engineering during the last decade have significantly enhanced the toolbox of enzymes available for chemical reactions, which may find application in the context of radiochemistry. In the present review, we intend to give an overview of the biocatalytic approaches that have been reported during the last four decades for the synthesis of PET radiotracers using Nitrogen-13, Carbon-11 and Fluorine-18...
December 12, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29230857/chemical-aspects-of-metal-ion-chelation-in-the-synthesis-and-application-antibody-based-radiotracers
#18
Eszter Boros, Jason P Holland
Radiometals are becoming increasingly accessible and are utilized frequently in the design of radiotracers for imaging and therapy. Nuclear properties ranging from the emission of γ-ray and ®+ -particles (imaging) to Auger electron, ®- and α-particles (therapy) in combination with long half-lives are ideally matched with the relatively long biological half-life of monoclonal antibodies in vivo. Radiometal labelling of antibodies requires the incorporation of a metal chelate onto the monoclonal antibody...
December 12, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29205456/automated-production-of-18-f-ftha-according-to-gmp
#19
Nina Savisto, Tapio Viljanen, Esa Kokkomäki, Jörgen Bergman, Olof Solin
14-(R,S)-[18 F]fluoro-6-thia-heptadecanoic acid is a tracer for fatty acid imaging by positron emission tomography. High demand for this tracer required us to replace semi-automatic synthesis with a fully automated procedure. An automated synthesis device was constructed in-house for multistep nucleophilic 18 F-fluorination and a control system was developed. The synthesis device was combined with a sterile filtration unit and both were qualified. 14-(R,S)-[18 F]fluoro-6-thia-heptadecanoic acid was produced according to good manufacturing practice guidelines set by the European Union...
December 4, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29143408/automated-synthesis-of-pet-radiotracers-by-copper-mediated-18-f-fluorination-of-organoborons-importance-of-the-order-of-addition-and-competing-protodeborylation
#20
Andrew V Mossine, Allen F Brooks, Vadim Bernard-Gauthier, Justin J Bailey, Naoko Ichiishi, Ralf Schirrmacher, Melanie S Sanford, Peter J H Scott
In this paper we describe the use of Cu-mediated [(18) F]fluorodeboronation for the automated production of PET radiotracers suitable for clinical use. Two recurrent issues with the method, low radiochemical conversion (RCC) on automation and protoarene byproduct purification issues, have been successfully addressed. The new method was utilized to produce sterile injectable doses of [(18) F]-(±)-IPMICF17, a PET radiotracer for tropomyosin receptor kinase B/C, using an automated synthesis module. Product was isolated in 1...
November 16, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
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