Journal of labelled compounds & radiopharmaceuticals最新文献_第2页

Practitioner Protocol for the Photoreduction of [14C]CO2 to [14C]CO and Its Application to the Aminocarbonylation of an Aryl Iodide [14C]CO2光还原为[14C]CO及其在芳基碘化氨基羰基化中的应用的实践规程

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-02-06 DOI: 10.1002/jlcr.70021

Quentin Lemesre, Augustin Malandain, Maxime Jay, David-Alexandre Buisson, Frédéric Taran, Antoine Sallustrau, Davide Audisio

{"title":"Practitioner Protocol for the Photoreduction of [14C]CO2 to [14C]CO and Its Application to the Aminocarbonylation of an Aryl Iodide","authors":"Quentin Lemesre, Augustin Malandain, Maxime Jay, David-Alexandre Buisson, Frédéric Taran, Antoine Sallustrau, Davide Audisio","doi":"10.1002/jlcr.70021","DOIUrl":"10.1002/jlcr.70021","url":null,"abstract":"<div>\u0000 \u0000 Carbon-14 labeling is fundamentally important for supporting the development of new agrochemicals and pharmaceuticals. Given its critical importance, continued innovation in technologies and methodologies for radiolabeling should be strongly encouraged to better support the radiochemistry community. However, a persistent gap often exists between technological breakthroughs and their broad adoption by the scientific community. To help bridge this gap, we have developed a Practitioner Protocol detailing a recent method from our laboratory. This protocol describes how to produce 14C-labeled carbon monoxide ([14C]CO) directly from the universal precursor, [14C]carbon dioxide ([14C]CO2). We hope this protocol will facilitate the adoption and implementation of this technology in other radiochemistry laboratories, thereby enhancing radiolabeling capabilities across the field.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 2","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146129751","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}

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Synthesis of Florasulam Stable Isotopes to Enable Identification of Degradants by Mass Spectrometry for Re-registration Studies 合成Florasulam稳定同位素，用质谱法鉴定降解物进行再登记研究。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-01-25 DOI: 10.1002/jlcr.70005

Caroline Long, Lindsey G. Horty

{"title":"Synthesis of Florasulam Stable Isotopes to Enable Identification of Degradants by Mass Spectrometry for Re-registration Studies","authors":"Caroline Long, Lindsey G. Horty","doi":"10.1002/jlcr.70005","DOIUrl":"10.1002/jlcr.70005","url":null,"abstract":"<div>\u0000 \u0000 Florasulam is a triazolopyrimidine herbicide that controls broadleaf and grass weeds in cereal crops and turf. It acts as an acetolactase synthase (ALS) inhibitor, blocking the synthesis of essential amino acids required for plant growth. Due to its potency, florasulam is effective at very low application rates making it cost-effective with reduced environmental off-target effects. As is common practice, florasulam has been subject to periodic reviews by regulatory agencies during re-registration requirements since its introduction into the market in 1998. The goal of these reviews is to ensure that the herbicide carries out its intended use without creating adverse side effects to humans and the environment. Since scientific methods are continually evolving and being developed, global regulatory agencies can require additional studies to address data gaps for pesticide renewals. During this re-registration process for florasulam, new environmental fate studies were conducted to meet new European Food Safety Authority (EFSA) guidelines. Consequently, florasulam-[triazole(13C,15N2)] and florasulam-[phenyl(13C6)] stable isotopes were synthesized to support the re-registration process.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 2","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-01-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146046378","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

Synthesis and Evaluation of Radioiodinated [125I]7-Iodo-5H-Pyrido[4,3-B]Indole ([125I]CTAU) in Postmortem Human Alzheimer's Disease Brain 放射性碘化[125I]7-碘- 5h -吡啶多[4,3- b]吲哚（[125I]CTAU）在人死后阿尔茨海默病脑中的合成与评价

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-01-10 DOI: 10.1002/jlcr.70003

Chloe C. McNamara, Agnes P. Biju, Emma Lynn M. Hipolito, Ngan T. B. Nguyen, Christopher Liang, Jogeshwar Mukherjee

{"title":"Synthesis and Evaluation of Radioiodinated [125I]7-Iodo-5H-Pyrido[4,3-B]Indole ([125I]CTAU) in Postmortem Human Alzheimer's Disease Brain","authors":"Chloe C. McNamara, Agnes P. Biju, Emma Lynn M. Hipolito, Ngan T. B. Nguyen, Christopher Liang, Jogeshwar Mukherjee","doi":"10.1002/jlcr.70003","DOIUrl":"10.1002/jlcr.70003","url":null,"abstract":"The aim of this study was to further understand the tau imaging agent, flortaucipir (T807), by making small modifications and assess its effect on tau protein binding in Alzheimer's disease (AD). Thus, the fluoropyridyl group in T807 was replaced with an iodine atom. We report here the development and preliminary evaluation of [125I]7-iodo-5H-pyrido[4,3-B]indole ([125I]CTAU) in postmortem AD brain slices. Using molecular docking, binding energies of CTAU indicated weaker tau binding compared with T807. In vitro tau binding assays in AD brain slices measured IC50 of CTAU and T807 as 44 × 10−9 M and 3.8 × 10−9 M, respectively. [125I]CTAU was synthesized in high radiochemical purity and molar activity (90 TBq/mmole). Binding of [125I]CTAU in the AD grey matter (GM) was observed, with lower nonspecific binding in the white matter (GM/WM = 2.3). Tau binding drugs (T807 and MK-6240, 10 μM) were both able to displace ~90% of bound [125I]CTAU in AD brain slices. Clorgyline (10 μM), a monoamine oxidase A inhibitor, decreased the binding of [125I]CTAU to 72% of total. In AD brain slices, [125I]CTAU exhibited a similar binding profile with the tau imaging agent [125I]IPPI. Although [125I]CTAU appears promising in vitro, any off-target issues need to be further studied to determine its use in AD-related dementias (ADRD).","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12789887/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145944470","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

Radiolabeling of Trastuzumab With Technetium-99m [99mTc] as a Radioligand for Screening Mentha pulegium on HER-2 Receptors 锝-99m [99mTc]放射标记曲妥珠单抗筛选HER-2受体上的脑膜炎

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-01-01 DOI: 10.1002/jlcr.70006

Narges Aryanpour, Golrokh Farnam, Farshad H. Shirazi, Soraya Shahhosseini

{"title":"Radiolabeling of Trastuzumab With Technetium-99m [99mTc] as a Radioligand for Screening Mentha pulegium on HER-2 Receptors","authors":"Narges Aryanpour, Golrokh Farnam, Farshad H. Shirazi, Soraya Shahhosseini","doi":"10.1002/jlcr.70006","DOIUrl":"https://doi.org/10.1002/jlcr.70006","url":null,"abstract":"<div>\u0000 \u0000 The use of medicinal plants as anti-cancer agents has attracted the attention of researchers. A method is needed for screening the anti-cancer effects on HER-2 receptors. In this study, a simple method based on radioligand binding studies was developed for primary screening of medicinal plants on HER-2 receptors in vitro. Trastuzumab was conjugated to HYNIC in a chemical reaction using NHS-HYNIC. HYNIC-Trastuzumab was radiolabeled with [99mTc] using SnCl2 as a reducing agent and tricine as a coligand. Biological activities of [99mTc]Tc-HYNIC-Trastuzumab were determined in saturation binding studies using the SKBR3 cell line. The IC50 of Mentha pulegium was determined in competition with [99mTc]Tc-HYNIC-Trastuzumab on the SKBR3 cell line. Radiochemical purity was ≥ 90% ± 2.08%. Based on the results, radiolabeled Trastuzumab maintained its biological activity after labeling (immunoreactivity = 83%, Kd = 7.049 ± 1.861 nM). The IC50 of Mentha pulegium was 31.3 ± 1.3 μg/mL. [99mTc]Tc-HYNIC-Trastuzumab can be used as a radioligand in competition binding studies for primary screening of medicinal plants, peptides, and small molecules in vitro on HER-2 receptors.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145887273","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

Antibody Drug Conjugate Formation Using 2-14C-Iminothiolane: A Radiochemical Analysis of Sequential Lysine Conjugation, Uncloaking of a Phantom Drug-to-Antibody Ratio, and Stability of the ADC 利用2- 14c -亚氨基硫烷形成抗体药物偶联物：序列赖氨酸偶联物的放射化学分析，揭示幻药-抗体比，以及ADC的稳定性。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-12-14 DOI: 10.1002/jlcr.70002

Michael Wallace, Michael J. Smith, John Brailsford, Difei Qiu, Alban J. Allentoff, Annie Tam, Selin Aytar, Michael Hay, Sharon Gong, Samuel Bonacorsi Jr.

{"title":"Antibody Drug Conjugate Formation Using 2-14C-Iminothiolane: A Radiochemical Analysis of Sequential Lysine Conjugation, Uncloaking of a Phantom Drug-to-Antibody Ratio, and Stability of the ADC","authors":"Michael Wallace, Michael J. Smith, John Brailsford, Difei Qiu, Alban J. Allentoff, Annie Tam, Selin Aytar, Michael Hay, Sharon Gong, Samuel Bonacorsi Jr.","doi":"10.1002/jlcr.70002","DOIUrl":"10.1002/jlcr.70002","url":null,"abstract":"<div>\u0000 \u0000 [14C]2-Iminothiolane ([14C]2-IT) served as a highly informative analytical tool to determine the rate of lysine thiolation and total addition of 2-IT to a monoclonal antibody. Specific activity measurements on [14C]2-IT modified mAbs found that lysine thiolation with 2-IT is linear regarding time and dependent on buffer strength. Conjugation with a fluorescent maleimide directly linked the free thiol-to-antibody ratio (FTAR) to the [14C]2-IT-to-antibody ratio ([14C]ITAR), providing accurate predictive information on the true number of sites proficient for payload conjugation and, by comparison with conjugation with the cytotoxic payload, quantified the absorbance from the nonconjugated cyclized N-substituted 2-iminothiolane adduct that created “phantom” drug-to-antibody ratios (PhDAR). Hydrolytic loss of the nonconjugated cyclized N-substituted 2-iminothiolane adduct was investigated using carbon-14 based radioquantitative HPLC, mass spectral analysis, and orthogonal [14C]ITAR and DAR measurements of the isolated [14C]mAb. These measurements combined to demonstrate that significant amounts of the cyclized products were shed from the [14C]ADC as [14C]thiobutyrolactone.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 14","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-12-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145756744","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

Assessment of Stability Extrapolation for Carbon-14 Labelled Compounds for the Determination of Extended Retest Periods 碳14标记化合物稳定性外推法测定延长复测周期的评价。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-12-14 DOI: 10.1002/jlcr.70000

Antonio Moreno-Herrera, Ryan A. Bragg, Charles S. Elmore

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Radiolabeled Aptamers for Bioimaging Applications in Oncology and Infectious Diseases 放射标记适体在肿瘤学和传染病生物成像中的应用。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-12-10 DOI: 10.1002/jlcr.70001

Najeeb Ullah, Tracy Ann Bruce-Tagoe, George Adu Asamoah, Shokoufeh Soleimani, Michael K. Danquah

{"title":"Radiolabeled Aptamers for Bioimaging Applications in Oncology and Infectious Diseases","authors":"Najeeb Ullah, Tracy Ann Bruce-Tagoe, George Adu Asamoah, Shokoufeh Soleimani, Michael K. Danquah","doi":"10.1002/jlcr.70001","DOIUrl":"10.1002/jlcr.70001","url":null,"abstract":"<div>\u0000 \u0000 Radiolabeled aptamers are promising molecular probes for bioimaging because of their potential for high specificity, stability, and rapid clearance from nontarget tissues. They are single-stranded oligonucleotides labeled with radionuclides such as technetium-99m (99ᵐTc), fluorine-18 (18F), and gallium-68 (68Ga) to enable precise imaging via single-photon emission computed tomography (SPECT) and positron emission tomography (PET). The versatility of radiolabeling strategies can provide opportunities to enhance biostability and pharmacokinetics while improving imaging sensitivity. In cancer theranostics, radiolabeled aptamers can allow early detection and treatment as well as facilitate effective monitoring of therapeutic responses. The applications of radiolabeled aptamers extend to infectious disease imaging, enabling real-time tracking of infections. Despite these advances, challenges such as rapid renal clearance, immunogenicity, and the need for clinical validation persist, catalyzing further research focused on enhancing the stability of radiolabeled aptamers, improving radiolabeling efficacy, and optimizing biodistribution. Emerging strategies, including nanoparticle conjugation and hybrid bioimaging, offer a great perspective for advancing the field. This article highlights recent advancements in radiolabeled aptamers in terms of their development, bioimaging applications, and research directions to address their limitations.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 14","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145723985","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

Abstracts From the 30th International Isotope Society UK Meeting 15th November 2024 第30届国际同位素学会英国会议摘要，2024年11月15日

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-11-26 DOI: 10.1002/jlcr.4165

引用次数: 0

Synthesis and Characterization of 2-Thiophenemethanamine-2H5 Hydrochloride 2-噻吩甲烷胺- 2h5盐酸盐的合成与表征

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-11-21 DOI: 10.1002/jlcr.4170

Sean David William Greenwood, Pete Deardorff, William Sherman, Desmond Slade

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Enhanced Control of Bacterial Wilt Disease in Tomato Plant via Transport and Penetration Tracking by Aid of 99mTc-Labeled Ralstonia solanacearum–Specific Bacteriophage 利用99mtc标记的番茄枯萎病特异性噬菌体的运输和渗透跟踪加强番茄青枯病的防治

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-11-11 DOI: 10.1002/jlcr.4169

Mohammed H. Abdel-Aal, Yasmeen A. Hasanien, Nahed A. Younis, Gamal El Didamony, Ahmed Askora, Gamal Abdelaziz

{"title":"Enhanced Control of Bacterial Wilt Disease in Tomato Plant via Transport and Penetration Tracking by Aid of 99mTc-Labeled Ralstonia solanacearum–Specific Bacteriophage","authors":"Mohammed H. Abdel-Aal, Yasmeen A. Hasanien, Nahed A. Younis, Gamal El Didamony, Ahmed Askora, Gamal Abdelaziz","doi":"10.1002/jlcr.4169","DOIUrl":"10.1002/jlcr.4169","url":null,"abstract":"<div>\u0000 \u0000 In order to reduce the development of antibiotic and chemical resistance in bacterial phytopathogens like Ralstonia solanacearum, which causes bacterial wilt disease, bacteriophages are a safe and efficient biocontrol method. This research will explore how to use radioisotopes to track the bacteriophage absorption by plants from roots to leaves as a means for improving phage persistence and thereby the control of bacterial wilt disease caused by R. solanacearum. We have investigated the uptake and delivery of R. solanacearum–specific bacteriophages in tomato plants. Transferring phage through roots to leaves showed a gradual increase over time until reaching the maximal at 120 min, where the percentage of bacteriophage reaches 21.95% of the total amount of the injected radiation dose, which is considered a good sign for the ability of bacteriophage to reach the leaves and infect the pathogen through its transport system if injected directly into soil. Demonstrating in-plant translocation of R. solanacearum–specific bacteriophages and their effect of reducing bacterial wilt symptoms may significantly contribute to a better control of R. solanacearum and promote further investigations on the penetration and translocation of phages into plants.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 13","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-11-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145488751","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