Journal of labelled compounds & radiopharmaceuticals最新文献_第4页

Improving Routine 89Zr-Immuno-PET Applications: Mild Iron Removal Can Favor the Use of Fe-DFO-N-suc-TFP Ester Over p-NCS-Bz-DFO 改进 89Zr-Immuno-PET 的常规应用：轻度除铁有利于使用 Fe-DFO-N-suc-TFP 酯而不是 p-NCS-Bz-DFO。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-05-14 DOI: 10.1002/jlcr.4097

Thomas E. Wuensche, Sabine Nauta, Guus A. M. S. van Dongen, Danielle J. Vugts

{"title":"Improving Routine 89Zr-Immuno-PET Applications: Mild Iron Removal Can Favor the Use of Fe-DFO-N-suc-TFP Ester Over p-NCS-Bz-DFO","authors":"Thomas E. Wuensche, Sabine Nauta, Guus A. M. S. van Dongen, Danielle J. Vugts","doi":"10.1002/jlcr.4097","DOIUrl":"10.1002/jlcr.4097","url":null,"abstract":"A key aspect for the applicability of 89Zr-radioimmunoconjugates is inert modification and radiolabeling. The two commercially available bifunctional variants of the siderophore desferrioxamine (DFO), Fe-DFO-N-suc-TFP-ester and p-NCS-Bz-DFO, are most often used for clinical 89Zr-immuno-PET. The use of Fe-DFO-N-suc-TFP-ester is advantageous with regard to higher radiolysis stability and more facile assessment of radiochemical purity as well as chelator-to-mAb ratio. However, not all mAbs withstand the Fe-removal step at relatively low pH (4–4.5) using EDTA, which is needed after conjugation to allow 89Zr labeling. In this study, it was investigated whether hydroxybenzyl ethylenediamine (HBED) or the clinically approved deferiprone (DFP) can serve as an alternative for EDTA to establish a pH-independent mild method for Fe-removal and thereby broaden the applicability of Fe-DFO-N-suc-TFP-ester. Carrier-added [59Fe]Fe-DFO-N-suc-TFP-ester was used for mAb modification to enable direct tracking of the Fe-removal efficiency under various conditions. Whereas incomplete Fe-removal with HBED was observed at pH 5 or higher, Fe-removal with DFP was possible at a broad pH range (4–9). This provides a mild, pH-independent method for Fe-removal, improving the applicability and attractiveness of Fe-DFO-N-suc-TFP-ester for 89Zr-mAb preparation.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 8","pages":"280-287"},"PeriodicalIF":0.9,"publicationDate":"2024-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4097","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140922445","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 Radiolabeled [14C]Rimsulfuron and Stable Isotope Labeled Rimsulfuron-[M + 3] to Support Crop Metabolism Studies for Reregistration 合成放射性标记的[14C]嘧磺隆和稳定同位素标记的嘧磺隆[M + 3]，以支持重新登记的作物代谢研究。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-05-06 DOI: 10.1002/jlcr.4096

Lindsey G. Horty, Timothy Martin

{"title":"Synthesis of Radiolabeled [14C]Rimsulfuron and Stable Isotope Labeled Rimsulfuron-[M + 3] to Support Crop Metabolism Studies for Reregistration","authors":"Lindsey G. Horty, Timothy Martin","doi":"10.1002/jlcr.4096","DOIUrl":"10.1002/jlcr.4096","url":null,"abstract":"<div>\u0000 \u0000 Rimsulfuron is a sulfonylurea herbicide that controls grass and broadleaf weeds in maize, potatoes, fruits, nuts, and other crops. It can also be used as a burndown herbicide to clear invasive weed species along roadsides and other nonagricultural land. Rimsulfuron acts as an acetolactase synthase (ALS) inhibitor, blocking the synthesis of essential amino acids required for plant growth. As is common practice, rimsulfuron has been subject to periodic reviews by regulatory agencies for reregistration since its introduction into the market in the early 1990s. 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 reregistration process for rimsulfuron, a new confined rotational crop study was required to address a data gap requested by the European Food Safety Authority (EFSA). Consequently, the corresponding pyridine and pyrimidine radiolabeled [14C]rimsulfuron and [M + 3] stable isotopes of rimsulfuron were synthesized for this study to support the reregistration process.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 7","pages":"263-272"},"PeriodicalIF":1.8,"publicationDate":"2024-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140864983","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

Efficient Reductive N-11C-Methylation Using Arylamines or Alkylamines and In Situ–Generated [11C]Formaldehyde From [11C]Methyl Iodide 使用芳基胺或烷基胺进行高效的 N-11C 甲基化还原反应，以及由 [11C]Methyl Iodide 原位生成 [11C]Formaldehyde

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-05-04 DOI: 10.1002/jlcr.4095

Tatsuya Kikuchi, Toshimitsu Okamura, Ming-Rong Zhang

{"title":"Efficient Reductive N-11C-Methylation Using Arylamines or Alkylamines and In Situ–Generated [11C]Formaldehyde From [11C]Methyl Iodide","authors":"Tatsuya Kikuchi, Toshimitsu Okamura, Ming-Rong Zhang","doi":"10.1002/jlcr.4095","DOIUrl":"10.1002/jlcr.4095","url":null,"abstract":"<div>\u0000 \u0000 Reductive N-11C-methylation using [11C]formaldehyde and amines has been used to prepare N-11C-methylated compounds. However, the yields of the N-11C-methylated compounds are often insufficient. In this study, we developed an efficient method for base-free reductive N-11C-methylation that is applicable to a wide variety of substrates, including arylamines bearing electron-withdrawing and electron-donating substituents. A 2-picoline borane complex, which is a stable and mild reductant, was used. Dimethyl sulfoxide was used as the primary reaction solvent, and glacial acetic acid or aqueous acetic acid was used as a cosolvent. While reductive N-11C-methylation efficiently proceeded under anhydrous conditions in most cases, the addition of water to the reductive N-11C-methylation generally increased the yield of the N-11C-methylated compounds. Substrates with hydroxy, carboxyl, nitrile, nitro, ester, amide, and phenone moieties and amine salts were applicable to the reaction. This proposed method for reductive N-11C-methylation should be applicable to a wide variety of substrates, including thermo-labile and base-sensitive compounds because the reaction was performed under relatively mild conditions (70°C) without the need for a base.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 7","pages":"254-262"},"PeriodicalIF":1.8,"publicationDate":"2024-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140829326","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

11C-Carbonylation for PET Imaging and Drug Discovery 用于 PET 成像和药物发现的 11C 碳酰化技术

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-05-01 DOI: 10.1002/jlcr.4094

Kenneth Dahl

引用次数: 0

Synthesis of Deuterated Endochin-Like Quinolones 氘代内脏类喹诺酮的合成。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-04-25 DOI: 10.1002/jlcr.4092

Sovitj Pou, Rolf W. Winter, Katherine M. Liebman, Rosie A. Dodean, Aaron Nilsen, Andrea DeBarber, J. Stone Doggett, Michael K. Riscoe

引用次数: 0

An Improved HPLC Separation Method for TSPO Radioligand [11C]ER176 Clinical Production 一种用于 TSPO 放射性配体 [11C]ER176 临床生产的改进型 HPLC 分离方法

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-04-19 DOI: 10.1002/jlcr.4093

Kang-Po Li, Hancheng Cai

{"title":"An Improved HPLC Separation Method for TSPO Radioligand [11C]ER176 Clinical Production","authors":"Kang-Po Li, Hancheng Cai","doi":"10.1002/jlcr.4093","DOIUrl":"10.1002/jlcr.4093","url":null,"abstract":"<div>\u0000 \u0000 Mitochondrial membrane translocator protein 18 kDa (TSPO) expression is increased in activated microglia, established as a plausible target of neuroinflammation imaging. [11C]ER176, specifically binding to TSPO, has been developed as the third generation of radioligand for PET imaging of TSPO, which showed the potential in better quantifying neuroinflammation than its predecessors. In the current study, we developed an automated radiosynthesis with an improved HPLC purification method for [11C]ER176 clinical production. The improved HPLC separation was integrated into the automated production of [11C]ER176 using a reverse phase semi-preparative HPLC column with an isocratic pump and the mixture of methanol and 50 mM ammonium acetate as the mobile phase. The fraction corresponding to [11C]ER176 was collected around 8.5–9.0 min without the risk of getting contaminations from nearby impurities. The automated production process took about 30 min after end of bombardment (EOB) and the quality of the final product [11C]ER176 met all specifications for clinical use based on current US Pharmacopeia and FDA CGMP requirements.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 7","pages":"273-276"},"PeriodicalIF":1.8,"publicationDate":"2024-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140626778","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

Carbon 14 and Carbon 13 Syntheses of Velagliflozin 碳 14 和碳 13 合成 Velagliflozin

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-04-11 DOI: 10.1002/jlcr.4091

Bachir Latli, Matt J. Hrapchak, Maxim Chevliakov, Chutian Shu

引用次数: 0

Preparation, Characterization, and Radiolabeling of Anti-HER2 scFv With Technetium Tricarbonyl and Stability Studies 三羰基锝抗 HER2 scFv 的制备、表征、放射性标记及稳定性研究

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-03-14 DOI: 10.1002/jlcr.4090

Negar Bozorgchami, Maryam Ahmadzadeh, Dara Hatamabadi, Abdolreza Yazdani, Soraya Shahhosseini, Elham Mohit

{"title":"Preparation, Characterization, and Radiolabeling of Anti-HER2 scFv With Technetium Tricarbonyl and Stability Studies","authors":"Negar Bozorgchami, Maryam Ahmadzadeh, Dara Hatamabadi, Abdolreza Yazdani, Soraya Shahhosseini, Elham Mohit","doi":"10.1002/jlcr.4090","DOIUrl":"10.1002/jlcr.4090","url":null,"abstract":"<div>\u0000 \u0000 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. 99mTc-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. We radiolabeled anti-HER2 scFv that was expressed in Escherichia coli and purified through Ni-NTA resin under native condition with 99mTc-tricarbonyl formed from boranocarbonate. HER2-based ELISA, BCA, TLC, and HPLC were used in this study. In the current study, anti-HER2 scFv was lyophilized before radiolabeling. It was found that freeze-drying did not change the binding activity of anti-HER2 scFv to HER2. Results demonstrated direct anti-HER2 scFv radiolabeling by 99mTc-tricarbonyl to hexahistidine sequence (His-tag) without any changes in biological activity and radiochemical purity of around 98%. Stability analysis revealed that 99mTc-anti-HER2 scFv is stable for at least 24 h in PBS buffer, normal saline, human plasma proteins, and histidine solution.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 5","pages":"168-179"},"PeriodicalIF":1.8,"publicationDate":"2024-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140131749","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 of Stable Isotope, Tritiated, and Carbon-14 Labeled Balcinrenone 合成稳定同位素、三联苯和碳-14 标记的 Balcinrenone。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-03-05 DOI: 10.1002/jlcr.4089

Jonas Bergare, Christopher Bailey, Henrik Sörensen, Gunnar Grönberg, Karl Broberg, Monica Berglund, Tudor Grecu, Carolina Sanchez, Hans Emtenäs, Ryan A. Bragg, Charles S. Elmore

引用次数: 0

Automated radiosynthesis of mGluR5 PET tracer [18F]FPEB from aryl-chloro precursor and validation for clinical application 从芳基氯前驱体中自动放射性合成 mGluR5 PET 示踪剂 [18 F]FPEB 并进行临床应用验证。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2024-02-19 DOI: 10.1002/jlcr.4088

Mahabuba Jahan, Arsalan Amir, Arindam Das, Jacob Kihlström, Sangram Nag

{"title":"Automated radiosynthesis of mGluR5 PET tracer [18F]FPEB from aryl-chloro precursor and validation for clinical application","authors":"Mahabuba Jahan, Arsalan Amir, Arindam Das, Jacob Kihlström, Sangram Nag","doi":"10.1002/jlcr.4088","DOIUrl":"10.1002/jlcr.4088","url":null,"abstract":"The radioligand [18F]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 [18F]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. [18F]FPEB was produced and isolated in high radioactivity and radiochemical purity. Throughout the validation process, thorough quality control measures are implemented. Radiopharmaceutical batch release criteria are established, including testing for physical appearance, filter integrity, pH, radiochemical purity, molar activity, radiochemical identity, chemical impurity, structural identity, stability, residual solvent, sterility, and endotoxin levels. In conclusion, the validation of [18F]FPEB involved a comprehensive process of synthesis optimization, quality control, which ensure the safety, efficacy, and quality of [18F]FPEB, enabling its reliable use in clinical PET. Here, we successfully radiolabeled and validated [18F]FPEB using aryl-chloro precursor according to GMP production for clinical application.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 4","pages":"155-164"},"PeriodicalIF":1.8,"publicationDate":"2024-02-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4088","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139900100","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