Journal of labelled compounds & radiopharmaceuticals最新文献

Synthesis of One Carbon-14 Labelled [14C-pyrazolo]-Ibrutinib 碳-14标记[14c -吡唑啉]-伊鲁替尼的合成。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-09-16 DOI: 10.1002/jlcr.4164

Pei Su, Bin Dong, Lei Xu, Zheng-Min Yang

{"title":"Synthesis of One Carbon-14 Labelled [14C-pyrazolo]-Ibrutinib","authors":"Pei Su, Bin Dong, Lei Xu, Zheng-Min Yang","doi":"10.1002/jlcr.4164","DOIUrl":"10.1002/jlcr.4164","url":null,"abstract":"<div>\u0000 \u0000 A safe and economical synthetic method for one new carbon-14 labelled 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-[14C-pyrazolo]-1Hpyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one, [14C-pyrazolo]-Ibrutinib (2) was prepared with [14C]-barium carbonate as starting material, achieving a total yield of 19% with radiochemical and chemical purities exceeding 98%. The synthesis pathway was compared with existing methods, particularly those described in Janssen's patent applications, which offer higher yields but with more complex synthetic processes and lower purity. Despite the existing literature reporting the synthesis of 13C-labelled Ibrutinib, the 14C labelled method described here provides a viable alternative, particularly in some application fields necessitating the radioactive isotopic tracer technique. This work underscores the ongoing need for improved synthetic routes that offer higher yields, milder reaction conditions, and lower costs in light of the growing interest in Ibrutinib due to its clinical efficacy and commercial potential.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 11-12","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145075115","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

Recent Advances in 11C-Labeling With [11C]CO2 for PET Imaging [11C]CO2在PET成像中的11C标记研究进展

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-09-08 DOI: 10.1002/jlcr.4162

Tianshuai Zhu, Jing-Jing Zhang, Lijun Tang, Zhen Chen

{"title":"Recent Advances in 11C-Labeling With [11C]CO2 for PET Imaging","authors":"Tianshuai Zhu, Jing-Jing Zhang, Lijun Tang, Zhen Chen","doi":"10.1002/jlcr.4162","DOIUrl":"10.1002/jlcr.4162","url":null,"abstract":"<div>\u0000 \u0000 Carbon-11 (11C)-labeled radiotracers are invaluable tools in positron emission tomography (PET), enabling real-time visualization of biochemical processes with high sensitivity and specificity. Among the various 11C synthons, cyclotron-produced [11C]CO2 is a fundamental precursor, though its direct incorporation into complex molecules has traditionally been limited by its low reactivity, gaseous form, and short half-life. Recent advances in [11C]CO2 fixation chemistry through both nonphotocatalytic and photocatalytic methods have significantly expanded its utility in the synthesis of structurally diverse compounds, including carboxylic acids, carbonates, carbamates, amides, and ureas. This review summarizes key developments in [11C]CO2 radiolabeling strategies, with critical evaluation of substrate scope, radiochemical yield, molar activity, and clinical translation potential. These advances collectively expand the synthetic versatility of [11C]CO2 and pave the way for the development of structurally diverse and clinically translatable PET imaging agents.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 11-12","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145012226","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

Hypoxia Inducible Factor-1α Specific Probe for Tumor Hypoxia Positron Emission Tomography Imaging 缺氧诱导因子-1α特异性探针用于肿瘤缺氧正电子发射断层成像

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-09-06 DOI: 10.1002/jlcr.4163

Qian Chen, Teli Liu, Xiaoyi Guo, Qian Zhang, Siqi Hao, Yang Jiang, Xianteng Yang, Nan Li, Hua Zhu, Zhi Yang

引用次数: 0

Synthesis and Preclinical Evaluation of ⁹⁹ᵐTc-HYNIC-Finasteride: A Novel SPECT Radiotracer Targeting 5α-Reductase in Prostate Cancer. 99 - tc - hynici -非那雄胺：一种靶向前列腺癌5α-还原酶的新型SPECT示踪剂的合成及临床前评价

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-09-01 DOI: 10.1002/jlcr.4167

Saba Shirin, Syed Qaiser Shah, Ralph Santos-Oliveira, Derya Ilem-Ozdemir

{"title":"Synthesis and Preclinical Evaluation of 99ᵐTc-HYNIC-Finasteride: A Novel SPECT Radiotracer Targeting 5α-Reductase in Prostate Cancer.","authors":"Saba Shirin, Syed Qaiser Shah, Ralph Santos-Oliveira, Derya Ilem-Ozdemir","doi":"10.1002/jlcr.4167","DOIUrl":"https://doi.org/10.1002/jlcr.4167","url":null,"abstract":"We describe the synthesis and preclinical assessment of a novel technetium-99m-labeled 5α-reductase (5AR) inhibitor, a 5AR-targeting drug, a target enzyme of prostate cancer (PCa) pathology, as a SPECT imaging probe. Finasteride was attached to 6-hydrazinonicotinic acid (HYNIC) with HYNIC NHS ester chemistry. The HYNIC-finasteride conjugate was identified by NMR, IR, MP analysis, high-resolution ESI MS ([M + H]+ m/z 507.3190, Δppm -3.9), and RP HPLC (Rt 13.9 min, > 98% purity). 99ᵐTc radiolabeling using tricine/EDDA co-ligands resulted in > 98% radiochemical purity. The radiotracer was highly stable in vitro (> 91% in PBS at 4 h; ≥ 68% in serum at 16 h) and had a logP value of -1.25 ± 0.08, with good hydrophilicity. Saturation binding assays in LNCaP cells had 5AR, with Kd and Bmax values of 3.10 ± 0.7 nM and 82.44 ± 3.2 fmol/106 cells. Biodistribution studies in LNCaP xenograft-bearing mice showed high tumor uptake (5.62% ± 0.32% ID/g at 4 h), which reduced in blocked groups (1.25% ± 0.18% ID/g). SPECT images offered selective tumor accumulation with good tumor-to-normal tissue contrast and renal clearance in tumor-bearing rabbits. These findings suggest that 99ᵐTc-HYNIC-finasteride is a promising SPECT radiotracer for noninvasive 5AR imaging in PCa.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 11-12","pages":"e4167"},"PeriodicalIF":0.9,"publicationDate":"2025-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145238793","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

Automated Manufacturing of Carbon-11 Radiopharmaceuticals Using Cassette-Based Radiosynthesizers. 使用盒式放射性合成器自动制造碳-11放射性药物。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-09-01 DOI: 10.1002/jlcr.4166

Michael L Schulte, Adam J Rosenberg

引用次数: 0

Automated Radiosynthesis of [18F]FMeNER-D2 Using the Simplified One-Pot 18F-Fluoromethylation Method 简化一锅18F-氟甲基化法自动放射合成[18F]FMeNER-D2

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-08-15 DOI: 10.1002/jlcr.4161

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

{"title":"Automated Radiosynthesis of [18F]FMeNER-D2 Using the Simplified One-Pot 18F-Fluoromethylation Method","authors":"Kazunori Kawamura, Wakana Mori, Yusuke Kurihara, Masanao Ogawa, Hiroki Hashimoto, Takayuki Ohkubo, Kaito Tsukagoe, Tomoya Fujishiro, Daisuke Arashi, Tatsuto Sato, Takeru Seki, Masatoshi Muto, Nobuki Nengaki, Masayuki Fujinaga, Ming-Rong Zhang","doi":"10.1002/jlcr.4161","DOIUrl":"10.1002/jlcr.4161","url":null,"abstract":"<div>\u0000 \u0000 (S,S)-2-(α-(2-[18F]Fluoro[dideutero]methoxyphenoxy)benzyl)morpholine ([18F]FMeNER-D2), which is used to image the norepinephrine transporter in the brain via positron emission tomography (PET), is typically radiosynthesized by O-fluoromethylating norethylreboxetine (NER) with [18F]bromofluoromethane-d2 using a fully automated 18F-labeling synthesizer with a two-pot unit. We simplified the automated radiosynthesis of [18F]FMeNER-D2 through the use of a straightforward one-pot method to prepare [18F]fluoromethyl-d2-tosylate as the fluoromethylating agent (avoiding the need to azeotropically dry [18F]F− in advance), which was then reacted with NER. The reaction conditions were optimized, with [18F]FMeNER-D2 synthesized using an 18F-labeling synthesizer equipped with a one-pot unit. As a result, a synthesis time, radiochemical yield based on total [18F]F−, molar activity, and radiochemical purity of 66 ± 4.7 min (n = 7), 9.0% ± 0.8% (n = 3), 130–275 GBq/μmol (n = 7), and > 97% (n = 7), respectively, were obtained at the end of synthesis. In conclusion, we successfully synthesized [18F]FMeNER-D2 using a simplified one-pot, fully automated, 18F-fluoromethylation method in an 18F-labeling synthesizer.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 9-10","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144843741","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

Influence of Activated Carbon on Fate of 14C-Sulfamethoxazole and 14C-Acetaminophen in Soil 活性炭对土壤中14c -磺胺甲恶唑和14c -对乙酰氨基酚归宿的影响

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-08-12 DOI: 10.1002/jlcr.4152

Kai Chen, Changfeng Yin, Juying Li

{"title":"Influence of Activated Carbon on Fate of 14C-Sulfamethoxazole and 14C-Acetaminophen in Soil","authors":"Kai Chen, Changfeng Yin, Juying Li","doi":"10.1002/jlcr.4152","DOIUrl":"10.1002/jlcr.4152","url":null,"abstract":"<div>\u0000 \u0000 In the present study, the influence of activated carbon (AC) on mineralization, degradation, extractable residues, and bound residue formation of 14C-sulfamethoxazole and 14C-acetaminophen was investigated. The results showed that AC facilitated the dissipation of 14C-sulfamethoxazole and 14C-acetaminophen and their formation of bound residue and exerted a significant inhibitory effect on their mineralization. The addition of 0.05%–2% AC showed an extraordinarily strong adsorption capacity of acetaminophen with Kd values of 47.2–409.8 times higher than that in the nonamended soil, as compared with 21.0–2273.4 times for sulfamethoxazole. An inverse relationship was found between sorption strength and mineralization or degradation kinetics. The effect of AC was likely due to its higher organic carbon (OC) content and the enhancement of surface areas and pore volumes where additional sites might be provided for binding or conjugation interactions with sulfamethoxazole or acetaminophen or their transformation products. Results from the present study clearly highlighted the significance of AC for influencing the fate of sulfamethoxazole and acetaminophen and stressed that sorption was potentially a critical factor in controlling the fate processes in soil.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 9-10","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144832821","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 [3H]muscimol [3H]麝香醇的合成

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-08-11 DOI: 10.1002/jlcr.4159

Michal Kriegelstein, Aleš Marek

{"title":"Synthesis of [3H]muscimol","authors":"Michal Kriegelstein, Aleš Marek","doi":"10.1002/jlcr.4159","DOIUrl":"10.1002/jlcr.4159","url":null,"abstract":"Muscimol, a potent GABAA receptor agonist and psychoactive alkaloid found in Amanita mushrooms, is widely used as a tool compound in neurochemical research. Despite its importance, synthetic access to [3H]muscimol of high specific activity has remained limited due to the challenges associated with conventional labeling strategies. Herein, we report a novel synthetic approach for the preparation of [3H]muscimol based on the reduction of a suitably protected amide precursor using in situ generated tritioborane (BT3·THF). The precursor was synthesized in four steps from dimethyl acetylenedicarboxylate, and subsequent electrophilic reduction afforded [3H]benzyl-protected muscimol in a radiochemical yield of 44 mCi (1.63 GBq) and a molar activity of 48.3 Ci/mmol (1.79 TBq/mmol). Final deprotection with HBr in acetic acid yielded [3H]muscimol·HBr in > 95% radiochemical purity. The method avoids the use of bulk tritiated water employed in established synthetic protocols and enables safe, reliable, and efficient access to this valuable radioligand for applications in GABA receptor studies.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 9-10","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4159","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144815059","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

99mTc-SNW-1 Nanoparticle Labeling and Its Biodistribution/Pathological Evaluations 99mTc-SNW-1纳米颗粒标记及其生物分布/病理评价

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-08-07 DOI: 10.1002/jlcr.4160

Setareh Derakhshan, Mehdi Shafiee Ardestani, Tahereh Zadeh Mehrizi, Ahmad Bitarafan-Rajabi, Safura Jokar, Morteza Pirali Hamedani, Mehdi Mirzaei

{"title":"99mTc-SNW-1 Nanoparticle Labeling and Its Biodistribution/Pathological Evaluations","authors":"Setareh Derakhshan, Mehdi Shafiee Ardestani, Tahereh Zadeh Mehrizi, Ahmad Bitarafan-Rajabi, Safura Jokar, Morteza Pirali Hamedani, Mehdi Mirzaei","doi":"10.1002/jlcr.4160","DOIUrl":"10.1002/jlcr.4160","url":null,"abstract":"<div>\u0000 \u0000 This study aimed to evaluate the targeted diagnostic imaging and therapeutic applications of SNW-1 nanoparticles. The nanoparticles were synthesized using microwave technique and characterized in terms of size, zeta potential, morphology, and chemical structure. The results demonstrated that the quasispherical and planar nanoparticles with the size of 370.4 nm and zeta potential of 0.4 mV were synthesized. Then, the nanoparticles were labeled with technetium-99m, and their in vivo biodistribution was assessed. Based on the results, the highest accumulation of the nanoparticles was observed in the bladder, liver, kidney, and heart tissues of the rabbits, respectively, while in the rat, the highest accumulation was observed in the liver, bladder, and heart tissues, respectively. In the rabbits, on average, the accumulation of the nanoparticles in the bladder was 7.4-, 8.7-, and 44.1-fold higher than that of the liver, kidney, and heart, respectively, while in the rat, the accumulation of the nanoparticles in the liver was 8.4- and 20.3-fold higher compared to that of the bladder and heart, respectively. The high bladder accumulation of the SNW-1 nanoparticles can be indicated by their high clearance, making them especially appropriate for kidney imaging and therapeutic applications.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 9-10","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144794638","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

C14-Labelled Synthesis of Benalaxyl-M and Its Two Soil Metabolites c14标记法合成苯丙醇- m及其两种土壤代谢物

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-08-04 DOI: 10.1002/jlcr.4157

Entela Sinani, Stefano Garau, Francesca Rizzo, Giovanni Meazza

引用次数: 0