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

Synthesis of Psilocin, Psilocybin and 5-MeO-DMT Succinate, All Labelled With Carbon-14 at the Indole 2-Position 吲哚2位碳-14标记裸盖菇素、裸盖菇素和5-MeO-DMT琥珀酸盐的合成

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-07-31 DOI: 10.1002/jlcr.4155

Rodney Brown, Niall M. Hamilton, Connor Mallon, James Stevenson, Michael T. Faley, Robert B. Kargbo, Alexander M. Sherwood, Balasubramaniam Upeandran

{"title":"Synthesis of Psilocin, Psilocybin and 5-MeO-DMT Succinate, All Labelled With Carbon-14 at the Indole 2-Position","authors":"Rodney Brown, Niall M. Hamilton, Connor Mallon, James Stevenson, Michael T. Faley, Robert B. Kargbo, Alexander M. Sherwood, Balasubramaniam Upeandran","doi":"10.1002/jlcr.4155","DOIUrl":"10.1002/jlcr.4155","url":null,"abstract":"<div>\u0000 \u0000 Three novel 14C-labelled isotopologues of the psychoactive agents psilocin, psilocybin and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) were synthesised, all labelled at the 2-position of the indole. The syntheses involved incorporating the 3-dimethylaminoethyl substituent common to all three substances onto a 4- or 5-substituted indole intermediate via successive treatments with oxalyl chloride, dimethylamine and reduction with lithium aluminium hydride.\u0000 Psilocybin-2-14C with a specific activity of 234 μCi/mg exhibited limited stability, but a 5.5-fold radio dilution with unlabelled psilocybin afforded material that maintained a radiochemical purity exceeding 97.5% after 1-month storage at ≤ −70°C. The stability of 5-MeO-DMT-2-14C succinate salt with a specific activity of 173 μCi/mg was assessed over a more extended storage period, and after 6 months at ≤ −70°C the radiochemical purity was 98.0%, supporting its use in long-term studies.\u0000 The radiolabelled psilocybin-2-14C and 5-MeO-DMT-2-14C succinate represent new tools for in vivo pharmacokinetic and metabolic studies with psychedelic tryptamines. These novel derivatives may offer enhanced metabolic stability and facilitate more precise ADME and mass balance studies. Future research will explore their behaviour in biological systems to support necessary studies toward regulatory approval of both psilocybin and 5-MeO-DMT for treating mental health disorders such as depression, anxiety and post-traumatic stress disorder.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 9-10","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144751561","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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Fully Automated Radiosynthesis of No-Carrier-Added [11C]Butanol Using the GE FASTLab 2 Module 使用GE FASTLab 2模块的无载载物添加[11C]丁醇的全自动放射合成

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-07-31 DOI: 10.1002/jlcr.4158

Ivan E. Wang, Jason A. Witek, Ryan J. Pakula, Bradford D. Henderson, Marianna Dakanali, Xia Shao, Peter J. H. Scott

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Synthesis of Two Versions of Carbon-14-Labeled ARV-110: An Androgen Receptor PROTAC Degrader for Prostate Cancer 两种碳-14标记ARV-110的合成：前列腺癌雄激素受体PROTAC降解剂

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-07-23 DOI: 10.1002/jlcr.4154

Xiang-Sheng Dai, Bin Dong, Lei Xu, Zheng-Min Yang

{"title":"Synthesis of Two Versions of Carbon-14-Labeled ARV-110: An Androgen Receptor PROTAC Degrader for Prostate Cancer","authors":"Xiang-Sheng Dai, Bin Dong, Lei Xu, Zheng-Min Yang","doi":"10.1002/jlcr.4154","DOIUrl":"10.1002/jlcr.4154","url":null,"abstract":"<div>\u0000 \u0000 N-((1R,4R)-4-(3-Chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide (ARV-110) is a proteolysis-targeting chimera (PROTAC) designed against the androgen receptor (AR), which shows great potential for treating AR-dependent diseases, such as prostate cancer. To support preclinical safety evaluations as well as studies of drug metabolism and pharmacokinetics, two versions of carbon-14-labeled ARV-110 were synthesized: N-((1R,4R)-4-(3-chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-[1,3-14C2]dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide (14C-ARV-110-a) and N-((1R,4R)-4-(3-chloro-4-[cyano-14C]cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide (14C-ARV-110-b). The synthesis of 14C-ARV-110-a was initiated from 1,2-dibromo-4,5-difluorobenzene and zinc cyanide-14C (Zn(14CN)₂), while 14C-ARV-110-b was prepared from 2-chloro-4-fluoro[cyano-14C]benzonitrile.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 9-10","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144688093","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 Radiolabeled and Stable-Isotope Labeled Deucravacitinib (BMS-986165) 放射性标记和稳定同位素标记Deucravacitinib （BMS-986165）的合成

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-07-22 DOI: 10.1002/jlcr.4156

John A. Brailsford, Kai Cao, Samuel J. Bonacorsi Jr.

引用次数: 0

Fully Automated Cassette-Based Production of [18F]Albumin Using the Trasis AllinOne Module 使用Trasis AllinOne模块全自动盒式生产[18F]白蛋白

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-07-05 DOI: 10.1002/jlcr.4153

Falguni Basuli, Jianfeng Shi, Xiang Zhang, Rolf E. Swenson

{"title":"Fully Automated Cassette-Based Production of [18F]Albumin Using the Trasis AllinOne Module","authors":"Falguni Basuli, Jianfeng Shi, Xiang Zhang, Rolf E. Swenson","doi":"10.1002/jlcr.4153","DOIUrl":"10.1002/jlcr.4153","url":null,"abstract":"<div>\u0000 \u0000 Fluorine-18 labeling of peptides and proteins is typically performed by an indirect labeling method. In this labeling approach, a labeled prosthetic group is prepared first and then conjugated to the proteins and peptides of interest. 6-[18F]fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester is a useful prosthetic group for indirect labeling. We have recently developed an efficient radiolabeling method, “fluorination on Sep-Pak,” that enables the preparation of this prosthetic group with high radiochemical yield and purity in under 10 min. A variety of biomolecules have been radiolabeled using this prosthetic group. The radiolabeling procedure was either manual or semiautomated. However, a fully automated synthesis method is essential for successful clinical translation. Therefore, we developed a fully automated reproducible radiolabeling method to prepare fluorine-18–labeled albumin using the Trasis AllinOne module. The procedure was completed in 50 min. The overall radiochemical yield was 25%–36% (decay-corrected, n = 6) using 1 mg of albumin with a radiochemical purity > 98%.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 9-10","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144558244","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

Thank You, Bob! 谢谢你，鲍勃！

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-06-16 DOI: 10.1002/jlcr.4151

引用次数: 0

Targeting VEGF With 99mTc-Labeled Ranibizumab for Noninvasive Diagnosis of Non-Small Cell Lung Cancer 99mtc标记的雷尼单抗靶向VEGF用于非小细胞肺癌的无创诊断

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-05-30 DOI: 10.1002/jlcr.4150

Muhammad Shehzad Saleem, Syed Qaiser Shah

{"title":"Targeting VEGF With 99mTc-Labeled Ranibizumab for Noninvasive Diagnosis of Non-Small Cell Lung Cancer","authors":"Muhammad Shehzad Saleem, Syed Qaiser Shah","doi":"10.1002/jlcr.4150","DOIUrl":"10.1002/jlcr.4150","url":null,"abstract":"<div>\u0000 \u0000 Angiogenesis, particularly driven by the overexpression of vascular endothelial growth factor (VEGF), plays a crucial role in the growth and metastasis of tumors, making VEGF a significant target in the diagnosis and therapy of non-small cell lung cancer (NSCLC). In this work, the potential of 99mTc-labeled ranibizumab was investigated for the non-invasive diagnosis of NSCLC. To that end, ranibizumab (RNB), a VEGF-neutralizing antibody, was conjugated with S-2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraaza1,4,7,10-tetra(2-carbamoylmethyl) cyclododecane (TCMC) followed by labeling with technetium-99m (99mTc) using different reaction parameters. The 99mTc-TCMC-RNB was characterized in terms of the percent radiochemical purity (% RCP) up to 6 h, in vitro stability in serum up to 16 h, internalization kinetics in A549 cells, and biodistribution using the NSCLC Sprague Dawley rat model. The 99mTc-labeled TCMC-RNB exhibited 98.3 ± 0.2% RCP in normal saline, stability in rat serum with an overall decay of 32.10% within 18 h, and specific binding to A549 NSCLC cells. Biodistribution studies showed significant tumor uptake. These findings suggest that 99mTc-labeled TCMC-RNB holds promise as a specific imaging agent for the diagnosis and monitoring of VEGF-related malignancies, particularly in NSCLC.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 7-8","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144171564","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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Correction to Validation of a Good Manufacturing Practice Procedure for the Production of [11C]AZD4747, a CNS Penetrant KRASG12c Inhibitor 对[11C]AZD4747（一种CNS渗透KRASG12c抑制剂）生产质量管理规范验证的更正

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-05-21 DOI: 10.1002/jlcr.4149

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Synthesis of a Potent Bruton's Tyrosine Kinase Inhibitor Labelled With Carbon-14 and Deuterium 碳-14 -氘标记布鲁顿酪氨酸激酶抑制剂的合成

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-05-05 DOI: 10.1002/jlcr.4148

Bachir Latli, Magnus Eriksson

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Ultrasound-Assisted Microcontinuous Process Facilitates the Selective Deuteration of Steroid Hormones 超声辅助微连续过程促进了类固醇激素的选择性氘化

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2025-05-05 DOI: 10.1002/jlcr.4146

Dan Wang, Xin Lv, Fang Wei

{"title":"Ultrasound-Assisted Microcontinuous Process Facilitates the Selective Deuteration of Steroid Hormones","authors":"Dan Wang, Xin Lv, Fang Wei","doi":"10.1002/jlcr.4146","DOIUrl":"10.1002/jlcr.4146","url":null,"abstract":"Constructing deuterated molecules efficiently and practically has been a long-standing challenge. Deuterated steroid hormones are essential for medical research and drug metabolism studies and are thus in high demand; mild and selective methods for the deuteration of steroid hormones have remained unexplored. Herein, we demonstrate a practical and efficient approach to synthesize 12 deuterated steroid hormones with up to 98% selectivity and 99% d-incorporation under an ultrasound-assisted microcontinuous process. Optical rotation experiments confirm that steroid hormones configurations are preserved during the H/D exchange reaction. Our protocol enables rapid, inexpensive, and sustainable gram-scale synthesis, facilitated by the reuse of deuterated solvents via molecular distillation technology. Applying synthetic deuterated steroid hormones as mass spectrometry standards, six steroid hormones in metabolites are accurately analyzed from Frozen Human Plasma-1950 sample. Overall, this work has successfully demonstrated the application of ultrasound assisted microcontinuous processing in enhancing H/D exchange reactions.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"68 5-6","pages":""},"PeriodicalIF":0.9,"publicationDate":"2025-05-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4146","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143909371","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