Journal of labelled compounds & radiopharmaceuticals最新文献_第6页

18F-Fluorination of a supported 2-(aryl-di-tert-butylsilyl)-N-methyl-imidazole for indirect 18F-labeling of a VHH single-variable domain 用于 VH H 单变量结构域间接 18 F 标记的 2-（芳基-二叔丁基硅基）-N-甲基咪唑的 18 F-氟化。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-01-15 DOI: 10.1002/jlcr.4082

Marine Steffann, Guillaume Bluet, Sébastien Roy, Catherine Aubert, Eric Fouquet, Philippe Hermange

引用次数: 0

Synthesis of [3H]Org24598 using in-house prepared [3H]MeI 使用内部制备的[3 H]MeI 合成[3 H]Org24598 。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-01-14 DOI: 10.1002/jlcr.4084

Michal Kriegelstein, Gabriela Nováková, Aleš Marek

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Preparation of [1′-13C]citric acid as a probe in a breath test to evaluate tricarboxylic acid cycle flux 制备[1'-13 C]柠檬酸作为呼气试验的探针，以评估三羧酸循环通量。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-01-03 DOI: 10.1002/jlcr.4083

Hidemichi Mitome, Mieko Takenishi, Kumiko Ono, Naoyuki Kawagoe, Tsunehiko Imai, Yosuke Sasaki, Yoshihisa Urita, Kazuki Akira

引用次数: 0

A facile synthesis of precursor for the σ-1 receptor PET radioligand [18F]FTC-146 and its radiofluorination σ-1受体PET放射性配体[18 F]FTC-146 前体的简易合成及其放射性氟化。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-01-03 DOI: 10.1002/jlcr.4081

Anna Marešová, Michal Jurášek, Pavel B. Drašar, Bohumil Dolenský, Elena A. Prokudina, Vladimir Shalgunov, Matthias M. Herth, Paul Cumming, Alexander Popkov

{"title":"A facile synthesis of precursor for the σ-1 receptor PET radioligand [18F]FTC-146 and its radiofluorination","authors":"Anna Marešová, Michal Jurášek, Pavel B. Drašar, Bohumil Dolenský, Elena A. Prokudina, Vladimir Shalgunov, Matthias M. Herth, Paul Cumming, Alexander Popkov","doi":"10.1002/jlcr.4081","DOIUrl":"10.1002/jlcr.4081","url":null,"abstract":"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 [18F]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. Herein, we present a simple one-step precursor synthesis followed by a one-step fluorine-18 labeling procedure that streamlines the preparation of [18F]FTC-146. Instead of a tosyl-based precursor, we developed a one-step synthesis of the precursor analog AM-16 containing a chloride leaving group for the SN2 reaction with 18F-fluoride. 18F-fluorination of AM-16 led to a moderate decay-corrected radiochemical yield (RCY = 7.5%) with molar activity (Am) of 45.9 GBq/μmol. Further optimization of this procedure should enable routine radiopharmaceutical production of this promising PET tracer.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 2","pages":"59-66"},"PeriodicalIF":1.8,"publicationDate":"2024-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4081","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139087222","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Open-source flow setup for rapid and efficient [18F]fluoride drying for automation of PET tracer syntheses 用于快速高效[18 F]氟化物干燥的开源流程设置，实现 PET 示踪剂合成自动化。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-12-28 DOI: 10.1002/jlcr.4080

Florian Menzel, Jonathan Cotton, Thomas Ziegler, Andreas Maurer, Jochen M. Neumaier

{"title":"Open-source flow setup for rapid and efficient [18F]fluoride drying for automation of PET tracer syntheses","authors":"Florian Menzel, Jonathan Cotton, Thomas Ziegler, Andreas Maurer, Jochen M. Neumaier","doi":"10.1002/jlcr.4080","DOIUrl":"10.1002/jlcr.4080","url":null,"abstract":"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. 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. This process relies on triflyl fluoride gas generation and allows nucleophilic [18F]fluoride to be prepared safely in a hotcell within 10 min and an activity recovery of 91.7 ± 1.6% (n = 5). Owing to the need for convenient radiofluorinated prosthetic ligands, we have adapted our continuous flow system to produce [18F]fluoroethyl tosylate (FEOTs) and [18F]fluoroethyl triflate (FEOTf), prosthetic groups that are widely used for late-stage fluoroethylation of PET tracers. The processes as well as the radiolabeling of different groups are compared and comprehensively discussed. Having a method providing [18F]fluoroethyl tosylate (FEOTs) as well as [18F]fluoroethyl triflate (FEOTf) quickly and highly efficiently is beneficial for radiochemical research.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 2","pages":"40-58"},"PeriodicalIF":1.8,"publicationDate":"2023-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4080","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139058439","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Development of radiotracers for riboflavin transporter 3 imaging in diseases—A brief overview 用于核黄素转运体 3 在疾病中成像的放射性racers 的开发--简述。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-12-22 DOI: 10.1002/jlcr.4076

Jindian Li, Xianzhong Zhang

引用次数: 0

Automated radiosynthesis of [18F]CETO, a PET radiotracer for imaging adrenal glands, on Synthra RNplus 用于肾上腺成像的 PET 放射性示踪剂 [18 F]CETO 在 Synthra RNplus 上的自动放射合成。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-12-20 DOI: 10.1002/jlcr.4078

Matthew Hird, Joseph J. Russell, Lei Li Corrigan, Istvan Boros, Patrik Nordeman, Gunnar Antoni, Mark Gurnell, Franklin I. Aigbirhio

{"title":"Automated radiosynthesis of [18F]CETO, a PET radiotracer for imaging adrenal glands, on Synthra RNplus","authors":"Matthew Hird, Joseph J. Russell, Lei Li Corrigan, Istvan Boros, Patrik Nordeman, Gunnar Antoni, Mark Gurnell, Franklin I. Aigbirhio","doi":"10.1002/jlcr.4078","DOIUrl":"10.1002/jlcr.4078","url":null,"abstract":"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 [18F]CETO to permit greater access to PA molecular imaging. Herein, we report an automated synthesis of this radiotracer. To manufacture the radiopharmaceutical routinely for clinical PET studies, we implemented an automated radiosynthesis method on a Synthra RNplus© synthesiser for which Cl-tosyletomidate was used as the precursor for radiolabelling via nucleophilic [18F]fluorination. [18F]CETO was produced with 35 ± 1% (n = 7), decay corrected and 25 ± 4% (n = 7) non-decay corrected radiochemical yield with molar activities ranging from 150 to 400 GBq/μmol. The GMP compliant manufacturing process produces a sterile formulated [18F]CETO injectable solution for human use as demonstrated by the results of quality control. Automation of the radiosynthesis of [18F]CETO should facilitate uptake by other adrenal centres and increase access to molecular imaging in PA.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 2","pages":"67-75"},"PeriodicalIF":1.8,"publicationDate":"2023-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4078","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138806677","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Validation of a good manufacturing practice procedure for the production of [11C]AZD4747, a CNS penetrant KRASG12c inhibitor 验证生产中枢神经系统穿透性 KRASG12c 抑制剂 [11C]AZD4747 的良好生产规范程序

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-12-20 DOI: 10.1002/jlcr.4079

Miguel A. Cortés González, Antonia A. Högnäsbacka, Christer Halldin, Magnus Schou

引用次数: 0

[11C]CO2 BOP fixation with amines to access 11C-labeled ureas for PET imaging 用胺固定[11C]CO2 BOP，获得用于 PET 成像的 11C 标记脲类

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-12-10 DOI: 10.1002/jlcr.4075

Coralie M. Bonnemaire, Albert D. Windhorst, Romano Orru, Eelco Ruijter, Danielle J. Vugts

{"title":"[11C]CO2 BOP fixation with amines to access 11C-labeled ureas for PET imaging","authors":"Coralie M. Bonnemaire, Albert D. Windhorst, Romano Orru, Eelco Ruijter, Danielle J. Vugts","doi":"10.1002/jlcr.4075","DOIUrl":"10.1002/jlcr.4075","url":null,"abstract":"Carbon-11 (11C) 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 11C-labeled tracers in humans.In this study, we present a novel and efficient method for the reaction of [11C]CO2 with amine precursors using benzotriazole-1-yl-oxy-tris-(dimethylamino)-phosphonium hexafluorophosphate (BOP) to access 11C-labeled ureas. Our method is extremely fast as it only requires transfer of [11C]CO2 into a solution with precursor and BOP at room temperature, where it reacts momentary into the desired 11C-labeled urea. This simple procedure makes it possible to radiolabel urea directly from [11C]CO2 without the need for advanced equipment, making the method applicable for all laboratories where [11C]CO2 is available. We synthesized a small series of aliphatic symmetrical and non-symmetrical 11C-labeled ureas using this method, and achieved good to excellent yields.The novelty of our study lies in the fact that peptide coupling reagent BOP is used for the first time in radiochemistry to activate [11C]CO2, facilitating its reaction with amines to obtain 11C-labeled ureas.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 6","pages":"201-210"},"PeriodicalIF":1.8,"publicationDate":"2023-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4075","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138627896","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

14C-radiolabeling of a new steroidal antiandrogen with a C-18 angular methyl extension 对带有 C-18 角甲基延伸的新型甾体抗雄激素进行 14C 放射标记

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-12-08 DOI: 10.1002/jlcr.4074

Jean-Yves Sancéau

引用次数: 0