Journal of labelled compounds & radiopharmaceuticals最新文献_第10页

A flow electrochemistry-enabled synthesis of 2-substituted N-(methyl-d)piperidines 流动电化学合成2-取代N-(甲基-d)哌啶

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-10-22 DOI: 10.1002/jlcr.4006

Azzam A. M. AL-Hadedi, Stuart Sawyer, Stuart J. Elliott, Robert A. Green, Daniel J. O'Leary, Richard C. D. Brown, Lynda J. Brown

引用次数: 0

In vivo and in vitro binding of [125I]I-R-(+)-TISCH: A dopamine D1 receptor ligand for studying pancreatic β-cell mass [125I]I-R-(+)- tisch:一种多巴胺D1受体配体在体内和体外结合研究胰腺β细胞质量

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-10-19 DOI: 10.1002/jlcr.4005

Yan Zhang, Guangwen Li, Yuli Sun, Haiyan Hong, Linlin Li, Yang Luo, Ran Wang, Lin Zhu, Hank F. Kung, Jinxia Zhu

{"title":"In vivo and in vitro binding of [125I]I-R-(+)-TISCH: A dopamine D1 receptor ligand for studying pancreatic β-cell mass","authors":"Yan Zhang, Guangwen Li, Yuli Sun, Haiyan Hong, Linlin Li, Yang Luo, Ran Wang, Lin Zhu, Hank F. Kung, Jinxia Zhu","doi":"10.1002/jlcr.4005","DOIUrl":"10.1002/jlcr.4005","url":null,"abstract":"Diabetes mellitus (DM) and insulinoma are mainly affected by the status of pancreatic β-cell mass (BCM). Development of imaging agents for BCM allows to study pancreatic β cells and the relationship between β cells and DM or insulinoma. In this study, we investigated the density of dopamine D1 receptor on the β cells and measured BCM by statistical image processing. The pancreatic uptakes of [125I]I-R-(+)-7-chloro-8-hydroxy-1-(3′-iodopheny1)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine ([125I]I-R-(+)-TISCH), dopamine D1 receptor tracer, in normal and diabetic rats displayed significant differences at 30 min (1.11 ± 0.08% ID/g vs. 0.63 ± 0.09% ID/g, p < 0.0001). In the presence of SCH23390, the pancreatic uptake of [125I]I-R-(+)-TISCH at 30 min in normal rats was lower (1.01 ± 0.04% ID/g, p < 0.05). Although the blocking was not complete, [125I]I-R-(+)-TISCH showed specific binding signals to the pancreas. Furthermore, the uptakes of [125I]I-R-(+)-TISCH in INS-1 cells were reduced in the presence of SCH23390 at different concentrations. [125I]I-R-(+)-TISCH displayed a respectable uptake in insulinoma. Overall, [125I]I-R-(+)-TISCH provided specific binding signals to pancreatic β cells. Although the specific signal may not be sufficient for imaging in vivo, the dopamine D1 receptor can still be considered as a potential target for studying BCM. Further investigation will be required to optimize the ligand.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10442209","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

Good manufacturing procedure production of [18F]SynVesT-1, a radioligand for in vivo positron emission tomography imaging of synaptic vesicle glycoprotein 2A 良好的生产程序生产[18F]SynVesT-1，一种用于突触囊泡糖蛋白2A体内正电子发射断层成像的放射配体

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-31 DOI: 10.1002/jlcr.4002

Kenneth Dahl, Stefan Larsson, Peter Bonn, Anita Wallin, Oleksiy Itsenko, Michael Schöll

{"title":"Good manufacturing procedure production of [18F]SynVesT-1, a radioligand for in vivo positron emission tomography imaging of synaptic vesicle glycoprotein 2A","authors":"Kenneth Dahl, Stefan Larsson, Peter Bonn, Anita Wallin, Oleksiy Itsenko, Michael Schöll","doi":"10.1002/jlcr.4002","DOIUrl":"10.1002/jlcr.4002","url":null,"abstract":"[18F]SynVesT-1 (also known as [18F]SDM-8 or [18F]MNI-1126) is a potent and selective synaptic vesicle glycoprotein 2 (SV2A) positron emission tomography (PET) imaging agent. In order to fulfill the increasing clinical demand of an 18F-labeled SV2A PET ligand, we have developed a fully automated procedure to provide a sterile and pyrogen-free good manufacturing procedure (GMP)-compliant product of [18F]SynVesT-1 suitable for clinical studies in humans. [18F]SynVesT-1 is synthesized via a rapid copper-mediated radiofluorination protocol. The procedure was developed and established on a commercially available module, TracerMaker (ScanSys Laboratorieteknik ApS, Copenhagen, Denmark), a synthesis platform originally developed to conduct carbon-11 radiochemistry. From ~130 GBq (end-of-bombardment), our newly developed procedure enabled us to prepare [18F]SynVesT-1 in an isolated radioactivity yield of 14,220 ± 800 MBq (n = 3), which corresponds to a radiochemical yield (RCY) of 19.5 ± 0.5%. The radiochemical purity (RCP) and enantiomeric purity of each of the final formulated batches exceeded 98%. The overall synthesis time was 90 min and the molar activity was 330 ± 60 GBq/μmol (8.9 ± 1.6 Ci/μmol). The produced [18F]SynVesT-1 was stable over 8 h at room temperature and is suitable for in vivo PET imaging studies in human subjects.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40334401","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

An improved radiosynthesis of [18F]FAraG, a PET radiotracer for imaging T-cell activation 一种用于成像t细胞激活的PET放射性示踪剂[18F]FAraG的改进放射合成

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-24 DOI: 10.1002/jlcr.3999

Daniel P. Holt, Robert F. Dannals

引用次数: 0

Low-scale syringe-made synthesis of 15N-labeled oligonucleotides 小型注射器合成15n标记的寡核苷酸

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-24 DOI: 10.1002/jlcr.4000

Břetislav Brož, František Tureček, Aleš Marek

引用次数: 1

Radiosynthesis and validation of [¹⁸ F]fluoroestradiol in a Synthra plus research platform for use in routine clinical practice. [18f]氟雌二醇在Synthra plus研究平台上的放射性合成和验证，用于常规临床实践。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-01 Epub Date: 2022-09-05 DOI: 10.1002/jlcr.3998

María Pía Pereira, María Emilia Tejería, Maia Zeni, Juan Pablo Gambini, Pablo Duarte, Ana Rey, Javier Giglio

{"title":"Radiosynthesis and validation of [18 F]fluoroestradiol in a Synthra plus research platform for use in routine clinical practice.","authors":"María Pía Pereira, María Emilia Tejería, Maia Zeni, Juan Pablo Gambini, Pablo Duarte, Ana Rey, Javier Giglio","doi":"10.1002/jlcr.3998","DOIUrl":"https://doi.org/10.1002/jlcr.3998","url":null,"abstract":"In this practitioner protocol, the optimization of the radiochemical synthesis of [18 F]fluoroestradiol (FES) on the Synthra RNplus research automated platform is described in detail and a quality control (QC) summary of three validation productions is presented. In comparison with published synthesis methods developed on other platforms, the yield was considerably improved (40%-45% ndc). The other important improvement is the reduction of the required concentration of H2 SO4 avoiding the production of high concentrations of acidic vapors that can deteriorate the module. Purification was achieved by solid phase extraction, and the required adaptation of an external heating plate to the module to evaporate the ethanol is also described. The product was obtained with high radiochemical purity and fulfilled all the requirements of current Good Manufacturing Practice (cGMP). The final product is formulated as a sterile, pyrogen-free solution suitable for human injection. To the best of our knowledge, this is the first report of FES production using this type of module.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40412169","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

Wiley Young Scientist Awards were handed over at the 14th International Symposium on the synthesis on the Synthesis and Applications of Isotopically Labelled Compounds in Raleigh, USA. 在美国罗利举行的第十四届同位素标记化合物合成与应用国际研讨会上颁发了Wiley青年科学家奖。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-01 Epub Date: 2022-08-24 DOI: 10.1002/jlcr.3995

Volker Derdau, Calum Novak-Mitchell

引用次数: 0

Highly effective liquid and solid phase extraction methods to concentrate radioiodine isotopes for radioiodination chemistry. 高效液相和固相萃取法浓缩放射性碘同位素，用于放射性碘化学。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-01 DOI: 10.1002/jlcr.3994

Christopher Davis, Chun Li, Ruirui Nie, Norman Guzzardi, Barbara Dworakowska, Pragalath Sadasivam, John Maher, Eric O Aboagye, Zhi Lu, Ran Yan

引用次数: 1

Comparison of three different methods in [⁶⁸ Ga]Ga-PSMA11 radiolabeling. [68 Ga]Ga- psma11放射性标记三种不同方法的比较

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-01 Epub Date: 2022-07-31 DOI: 10.1002/jlcr.3993

Doğangün Yüksel, Ayşe Uğur

{"title":"Comparison of three different methods in [68 Ga]Ga-PSMA11 radiolabeling.","authors":"Doğangün Yüksel, Ayşe Uğur","doi":"10.1002/jlcr.3993","DOIUrl":"https://doi.org/10.1002/jlcr.3993","url":null,"abstract":"In this study, quality control parameters such as radiochemical yield, radiochemical purity, and in vitro stability of gallium (68 Ga)-prostate-specific membrane antigen-11 ([68 Ga]Ga-PSMA11) radiopharmaceutical obtained in a research laboratory with three different synthesis algorithms were evaluated and compared. Gallium (68 Ga) chloride precursor to be used in labeling in all three methods was obtained by using ITG brand 68 Ge/68 Ga generator. The first method for the [68 Ga]Ga-PSMA11 radiopharmaceutical was performed with the automated synthesis module, which is widely used in clinical practice. Its radiochemical yield, quality assurance, and stability met expectations. Radiolabeling success, suitability of quality control parameters, and in vitro stability of [68 Ga]Ga-PSMA11 radiopharmaceutical performed with ANMI kit were examined. The final product showed success in 68 Ga-complexation kinetics. All quality control criteria performed met the expectation for clinical applications. Direct cold labeling of PSMA11 ligand with sodium bicarbonate buffer was examined. Results were similar to the ANMI kit. Considering that all three methods are successful in radiochemical labeling, labeling with NaHCO3 buffer shows the labeling preference when we choose the cheap, practical, and easy labeling option.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40532562","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: 1

Simplified and accessible [¹⁸ F]F-AraG synthesis procedure for preclinical PET. 临床前PET的F- arag合成过程的简化和易于获取[18 F]。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-01 DOI: 10.1002/jlcr.3997

Antonia A Högnäsbacka, Miguel A Cortés González, Christer Halldin, Magnus Schou

引用次数: 1