Journal of labelled compounds & radiopharmaceuticals最新文献

Reliable One-Pot Automated Preparation of [11C]SL25.1188 for Use in Clinical Imaging Studies 可靠的一锅自动制备[11C]SL25.1188用于临床影像学研究

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-08-21 DOI: 10.1002/jlcr.70035

Hiroki Hashimoto, Takayuki Ohkubo, Kaito Tsukagoe, Tomoya Fujishiro, Daisuke Arashi, Tatsuto Sato, Takeru Seki, Yusuke Kurihara, Masanao Ogawa, Masatoshi Muto, Nobuki Nengaki, Wakana Mori, Masayuki Fujinaga, Kazunori Kawamura, Ming-Rong Zhang

{"title":"Reliable One-Pot Automated Preparation of [11C]SL25.1188 for Use in Clinical Imaging Studies","authors":"Hiroki Hashimoto, Takayuki Ohkubo, Kaito Tsukagoe, Tomoya Fujishiro, Daisuke Arashi, Tatsuto Sato, Takeru Seki, Yusuke Kurihara, Masanao Ogawa, Masatoshi Muto, Nobuki Nengaki, Wakana Mori, Masayuki Fujinaga, Kazunori Kawamura, Ming-Rong Zhang","doi":"10.1002/jlcr.70035","DOIUrl":"https://doi.org/10.1002/jlcr.70035","url":null,"abstract":"<div>\u0000 \u0000 We clinically investigated (S)-5-methoxymethyl-3-[6-(4,4,4-trifluorobutoxy)benzo[d]isoxazol-3-yl]oxazolidin-2-[11C]-one ([11C]SL25.1188) as a positron emission tomography tracer for imaging monoamine oxidase B. To perform clinical imaging studies at our institute, we established a routine method for preparing the [11C]SL25.1188 injection using a one-pot [11C]CO2 fixation method. We successfully prepared the [11C]SL25.1188 injection using a 11C-labeling synthesizer and sterile isolator. The radiosynthesis time and decay-corrected radiochemical yield based on [11C]CO2 were below 30 min and 49% ± 10% postirradiation (n = 104), respectively. At the end of synthesis (n = 104), the molar activity was 180 ± 57 GBq/μmol, and the radiochemical purity exceeded 99%. The results of [11C]SL25.1188 injection complied fully with our in-house quality control and quality assurance criteria, confirming a reliable supply of high-quality [11C]SL25.1188 formulation with adequate radioactivity for use in clinical imaging studies.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148784742","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Gram-Scale Synthesis of Perdeuterated Paracetamol 克级合成过氘化扑热息痛

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-08-04 DOI: 10.1002/jlcr.70034

Alexander Park, Robert M. Edkins, June McCorquodale, James Tellam, Sarah Youngs, Katharina Edkins

{"title":"Gram-Scale Synthesis of Perdeuterated Paracetamol","authors":"Alexander Park, Robert M. Edkins, June McCorquodale, James Tellam, Sarah Youngs, Katharina Edkins","doi":"10.1002/jlcr.70034","DOIUrl":"https://doi.org/10.1002/jlcr.70034","url":null,"abstract":"The synthesis of deuterated compounds is a major stumbling block in the field of neutron total scattering on disordered materials. This is due to the requirement for large quantities of pure sample with high deuterium content across all positions. Typical deuterations in literature focus on site-specific deuterations typically on milligram scales. Here, we successfully synthesised paracetamol-d9, as well as its related isotopologues, on a multigram scale. We proceeded through an acid-catalysed deuteration of 4-aminophenol under microwave irradiation. We were able to efficiently purify the unstable intermediate, 4-aminophenol-d4 by sublimation, which meant we could avoid the formation of strongly coloured impurities that could not be removed from the final product otherwise. The pure intermediate then underwent acetylation with a 75% yield. More than 10 g of the final perdeuterated product was synthesised with an average deuterium incorporation of > 93% and no less than 78% at any individual position.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-08-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.70034","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148662478","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

Synthesis and Characterization of 2-(1-Hydroxyethyl)Promazine Sulfoxide-d₄ HCl as an Internal Standard for the Accurate Quantitation of 2-(1-Hydroxyethyl)Promazine Sulfoxide in Equine Urine. 2-（1-羟乙基）丙嗪亚砜-d4 HCl的合成及表征作为马尿中2-（1-羟乙基）丙嗪亚砜准确定量的内标

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-08-01 DOI: 10.1002/jlcr.70036

Justin C Holmes, Ballard C Smith, Samuel G Awuah, Rodney Eisenberg, Andreas F Lehner, Clara K Fenger, George A Maylin, Kimberly Brewer, Thomas Tobin

{"title":"Synthesis and Characterization of 2-(1-Hydroxyethyl)Promazine Sulfoxide-d4 HCl as an Internal Standard for the Accurate Quantitation of 2-(1-Hydroxyethyl)Promazine Sulfoxide in Equine Urine.","authors":"Justin C Holmes, Ballard C Smith, Samuel G Awuah, Rodney Eisenberg, Andreas F Lehner, Clara K Fenger, George A Maylin, Kimberly Brewer, Thomas Tobin","doi":"10.1002/jlcr.70036","DOIUrl":"10.1002/jlcr.70036","url":null,"abstract":"Acetylpromazine, 1-{10-[3-(dimethylamino)propyl]-10H-phenothiazin-2-yl}ethenone, C19H22N2OS, 326.46 g·mol-1 is a phenothiazine derivative at one time used in human medicine as an antipsychotic medication but now predominantly used in veterinary medicine as a sedative/tranquilizer and referred to as acepromazine. In performance horses its use is regulated by using a 10 ng/mL threshold for the major urinary metabolite 2-(1-hydroxyethyl) promazine-sulfoxide (HEPS) in equine urine. To enable accurate quantitation of HEPS in equine urine we have synthesized and purified hydroxyethylpromazine sulfoxide-d4 (HEPS-d4) to be used as a stable isotopically labeled internal standard. Although labeled HEPS is commercially available (CAS 1346605-30-8), to the best of our knowledge there is no published synthetic procedure in the scientific literature. Here we demonstrate a viable synthetic procedure consisting of four major steps: (i) freebasing the Acepromazine maleate salt, (ii) H-D exchange of Acepromazine at room temperature, (iii) reduction of the ketone with NaBD4, and (iv) oxidation of the thioether via hydrogen peroxide and acetic acid. This deuterated internal standard will allow for precise LC/MS quantitation of HEPS at regulatory threshold concentrations, enabling accurate detection and quantitation of picogram/mL concentrations in equine urine samples, thereby supporting regulatory compliance for equine medication control programs.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":"e70036"},"PeriodicalIF":1.3,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13531255/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148865371","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

Synthesis of Potent Vanin-1 Inhibitors Labelled With Carbon-14 and Deuterium 碳-14和氘标记强效Vanin-1抑制剂的合成。

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-07-09 DOI: 10.1002/jlcr.70033

Bachir Latli, Matt Hrapchak, Ling Wu, Lalith Samankumara, Jaehee Lee, Bo Qu

{"title":"Synthesis of Potent Vanin-1 Inhibitors Labelled With Carbon-14 and Deuterium","authors":"Bachir Latli, Matt Hrapchak, Ling Wu, Lalith Samankumara, Jaehee Lee, Bo Qu","doi":"10.1002/jlcr.70033","DOIUrl":"10.1002/jlcr.70033","url":null,"abstract":"<div>\u0000 \u0000 Vanin-1 is an enzyme highly expressed in the kidneys, liver, and small intestines. Inhibition of this enzyme has been postulated as a novel approach in the treatment of several inflammatory diseases. BI 764122, BI 1585773, and BI 1595043 are very potent inhibitors of this enzyme. These three analogs share the same (S)-N-(nicotinoyl)pyrrolidin-3-yl)-N-methyl acetamide moiety. The preparation of these analogs labelled with carbon-14 was accomplished via carbon-14 carboxylation with carbon dioxide of corresponding aryl halides, followed by amide bond formation with (S)-N-(methyl)-N-(pyrrolidin-3-yl)acetamide. For metabolic considerations, the radioactive carbon was also incorporated in a cyclopropyl in [14C]-BI 764122 synthesis. The deuterium labelling of these three compounds was completed using the common moiety (S)-N-(methyl-d3)-N-(pyrrolidin-3-yl)acetamide-d3, which was prepared in three steps and then coupled to the corresponding aryl acids via amide bond.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 9","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148411973","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A 64Cu-Labeled Oxopurine Derivative for Translocator Protein–Targeted Inflammation Imaging 用于转位蛋白靶向炎症成像的64cu标记的氧嘌呤衍生物。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-06-02 DOI: 10.1002/jlcr.70032

Undram Ochirsukh, Iqra Bibi, Ho Young Kim, In Ok Ko, Kyung Jun Kang, Hyun Ji Lee, Kwang Il Kim, Ji-Ae Park, Jung Young Kim

{"title":"A 64Cu-Labeled Oxopurine Derivative for Translocator Protein–Targeted Inflammation Imaging","authors":"Undram Ochirsukh, Iqra Bibi, Ho Young Kim, In Ok Ko, Kyung Jun Kang, Hyun Ji Lee, Kwang Il Kim, Ji-Ae Park, Jung Young Kim","doi":"10.1002/jlcr.70032","DOIUrl":"10.1002/jlcr.70032","url":null,"abstract":"<div>\u0000 \u0000 The translocator protein (TSPO) is a mitochondrial biomarker overexpressed in activated immune cells and various tumors that is an attractive target for positron emission tomography (PET) imaging of inflammation and the tumor microenvironment. We designed and evaluated the novel TSPO-targeted PET tracer, 64Cu-purine ([64Cu]5), constructed from a purine scaffold conjugated to a NOTA chelator. Molecular docking analysis indicated that the DOTA analog exhibited slightly higher TSPO binding affinity than did the NOTA derivative; however, the NOTA chelator was selected for 64Cu labeling due to its superior radiochemical yield and stability. [64Cu]5 demonstrated high radiochemical purity, excellent in vitro and in vivo stability, and moderate lipophilicity, which minimized nonspecific uptake. In vitro, [64Cu]5 showed significantly higher uptake in inflammatory macrophages than in tumor cells. In vivo PET imaging and biodistribution studies revealed preferential accumulation in inflamed and tumor tissues, with reduced uptake following PK11195 administration. Autoradiography and immunohistochemistry confirmed tracer accumulation in both inflamed and tumor tissues, reflecting the presence of inflammation within the tumor microenvironment. Overall, these findings suggest that [64Cu]5 is a promising TSPO-targeting PET radiotracer for imaging inflammation-associated processes in tumors.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 7-8","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148143680","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Fully Automated Production of Multiple 11C-Labeled PET Tracers Using a Self-Cleaning TracerMaker Radiosynthesizer 全自动生产多个11c标记PET示踪剂使用自清洁示踪机放射性合成器。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-05-15 DOI: 10.1002/jlcr.70031

Bao Hu, Wenchao Qu, Ramin Parsey, Mark Slifstein, Peter Larsen

{"title":"Fully Automated Production of Multiple 11C-Labeled PET Tracers Using a Self-Cleaning TracerMaker Radiosynthesizer","authors":"Bao Hu, Wenchao Qu, Ramin Parsey, Mark Slifstein, Peter Larsen","doi":"10.1002/jlcr.70031","DOIUrl":"10.1002/jlcr.70031","url":null,"abstract":"<div>\u0000 \u0000 The rapid translation of carbon-11 PET radiotracers into clinical and preclinical research requires automated synthesis modules capable of fast, reliable, and reproducible production. Here, we report the development and application of a fully automated TracerMaker radiosynthesizer for routine production of multiple 11C-labeled PET tracers at the PET Research Core, Stony Brook University. The system integrates automated Sep-Pak preconditioning, in-line sterile filter integrity testing, and a fully automated postproduction cleaning protocol that significantly reduces operator workload and radiation exposure. Using this module, three radiotracers with high clinical research interest, (E)-3-(6-methyl-pyridin-2-ylethynyl)-cyclohex-2-enone-O-11C-methyl-oxime ((E)-[11C]ABP688), 5-(4-(Methoxy-11C)phenyl)-1-(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazole ([11C]PS13), and 11C-labeled Pittsburgh Compound B ([11C]PiB) were successfully produced without hardware modification. The automated cleaning protocol enables rapid turnaround between runs and supports high-throughput sequential production. These results demonstrate that the TracerMaker module provides a robust, flexible, and cost-effective platform for the routine clinical production of carbon-11 radiopharmaceuticals.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 4-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147948709","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-05-15

引用次数: 0

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-05-15

引用次数: 0

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-21

引用次数: 0

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-04-21

引用次数: 0