Journal of Labelled Compounds and Radiopharmaceuticals 
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This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.Carbon ‐13 labeling of ibrutinib for human microdosing
A 10-step, gram-scale production of carbon-13 labeled ibrutinib from [13C6]phenol was accomplished in 31% overall yield with>99% chemical purity and>99% enantiomeric excess (ee), suitable for intravenous microdosing in humans. Ibrutinib is an oral medication for the treatment of B cell malignancies. During its clinical development, a stable isotopologue of ibrutinib was required for the assessment of the drug's absolute oral bioavailability via intravenous microdosing. The following work describes a 10-step, gram-scale production of carbon-13 labeled ibrutinib from [13C6]phenol (13C6, 99%) in 31% overall yield with&g...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 1, 2022 Category: Biochemistry Authors: Yong Gong,
Rhys Salter Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research
Carbon ‐13 labeling of ibrutinib for human microdosing
Ibrutinib is an oral medication for the treatment of B cell malignancies. During its clinical development, a stable isotopologue of ibrutinib was required for the assessment of the drug ’s absolute oral bioavailability via intravenous microdosing. The following work describes a ten-step, gram-scale production of carbon-13 labeled ibrutinib from [13C6]phenol (13C6, 99%) in 31% overall yield with>99% chemical purity and>99% enantiomeric excess (ee), suitable for intravenous microdosing in humans. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - November 23, 2022 Category: Biochemistry Authors: Yong Gong,
Rhys Salter Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research
Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - November 16, 2022 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research
A flow electrochemistry ‐enabled synthesis of 2‐substituted N‐(methyl‐d)piperidines
Synthesis ofN-monodeuteriomethyl-2-substituted piperidines by efficient and scalable methoxylation ofN-formylpiperidine in an electrochemical flow cell, followed by an Eschweiler –Clarke reaction with formic acid-d2 and unlabelled formaldehyde, is described. These monodeuteratedN-methyl possess small isotropic proton chemical shift differences important in the investigation of molecules that are able to support long-lived nuclear spin states in solution NMR. A synthesis ofN-monodeuteriomethyl-2-substituted piperidines is described. An efficient and readily scalable anodic methoxylation ofN-formylpiperidine in an undivide...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - November 15, 2022 Category: Biochemistry Authors: Azzam A. M. AL ‐Hadedi,
Stuart Sawyer,
Stuart J. Elliott,
Robert A. Green,
Daniel J. O'Leary,
Richard C. D. Brown,
Lynda J. Brown Tags: RESEARCH ARTICLE Source Type: research
In vivo and in vitro binding of [125I]I ‐R‐(+)‐TISCH: A dopamine D1 receptor ligand for studying pancreatic β‐cell mass
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 block...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - November 7, 2022 Category: Biochemistry Authors: Yan Zhang,
Guangwen Li,
Yuli Sun,
Haiyan Hong,
Linlin Li,
Yang Luo,
Ran Wang,
Lin Zhu,
Hank F. Kung,
Jinxia Zhu Tags: RESEARCH ARTICLE Source Type: research
A Flow Electrochemistry ‐Enabled Synthesis of 2‐Substituted N‐(Methyl‐d)piperidines
A synthesis ofN-monodeuteriomethyl-2-substituted piperidines is described. An efficient and readily scalable anodic methoxylation ofN-formylpiperidine in an undivided microfluidic electrolysis cell delivers methoxylated piperidine 3, which is a precursor to aN-formyliminium ion and enables C-nucleophiles to be introduced at the 2-position. The isotopically labelledN-deuteriomethyl group is installed using the Eschweiler-Clarke reaction with formic acid-d2 and unlabelled formaldehyde. MonodeuteratedN-methyl groups in these molecular systems possess small isotropic proton chemical shift differences important in the investiga...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - October 23, 2022 Category: Biochemistry Authors: Azzam A. M. AL ‐Hadedi,
Stuart Sawyer,
Stuart J. Elliott,
Robert A. Green,
Daniel J. O’Leary,
Richard C. D. Brown,
Lynda J. Brown Tags: RESEARCH ARTICLE Source Type: research
In vivo and in vitro binding of [125I]I ‐R‐(+)‐TISCH: a dopamine D1 receptor ligand for studying pancreatic β‐cell mass
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/gvs 0.63 ± 0.09% ID/g,P< 0.0001). In 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-(+)-...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - October 20, 2022 Category: Biochemistry Authors: Yan Zhang,
Guangwen Li,
Yuli Sun,
Haiyan Hong,
Linlin Li,
Yang Luo,
Ran Wang,
Lin Zhu,
Hank F. Kung,
Jinxia Zhu Tags: RESEARCH ARTICLE Source Type: research
Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - October 14, 2022 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research
The impact of zirconium ‐89 solution formulation on the efficiency of [89Zr]Zr‐deferoxamine synthesis
This article provides the results of a comparative study of methods for obtaining89Zr solutions using ZR, Chelex-100, and TBP resins in the form of [89Zr]Zr-oxalate, [89Zr]Zr-chloride, and [89Zr]Zr-citrate in terms of purification and labeling efficiency. All evaluated methods allowed us to obtain89Zr with high yield (>90% in 1 ml). The chemical form of89Zr has a significant influence on the radiolabeling efficiency of the deferoxamine (DFO) chelator and its derivatives. Compared with [89Zr]Zr-oxalate, the application of [89Zr]Zr-chloride and [89Zr]Zr-citrate solutions leads to a higher efficacy of [89Zr]Zr-DFO compl...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - October 11, 2022 Category: Biochemistry Authors: Viktor Bubenshchikov,
Artur Makichyan,
Anton Larenkov Tags: RESEARCH ARTICLE Source Type: research
A practical approach to the optimization of positron emission tomography imaging agents for the central nervous system
The discovery of novel imaging agents for positron emission tomography (PET) relies on medicinal chemistry best practices, including a good understanding of molecular and pharmacological properties required for the acquisition of relevant, high-quality images. This short note reviews the characteristics of a series of clinically successful imaging agents, providing guidance for the optimization of such molecular tools. PET imaging plays an important role in staging disease and in helping clinical dose selection, which is critical for the efficient development of drug candidates. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 30, 2022 Category: Biochemistry Authors: Yves P. Auberson,
Akan é Lièvre,
Sandrine Desrayaud,
Emmanuelle Briard Tags: SHORT NOTE Source Type: research
A practical approach to the optimization of positron emission tomography (PET) imaging agents for the central nervous system
The discovery of novel imaging agents for positron emission tomography (PET) relies on medicinal chemistry best practices, including a good understanding of molecular and pharmacological properties required for the acquisition of relevant, high-quality images. This short note reviews the characteristics of a series of clinically successful imaging agents, providing guidance for the optimization of such molecular tools. PET imaging plays an important role in staging disease and in helping clinical dose selection, which is critical for the efficient development of drug candidates. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 23, 2022 Category: Biochemistry Authors: Yves P. Auberson,
Akan é Lièvre,
Sandrine Desrayaud,
Emmanuelle Briard Tags: SHORT NOTE Source Type: research
The impact of zirconium ‐89 solution formulation on the efficiency of [89Zr]Zr‐DFO synthesis
This article provides the results of a comparative study of methods for obtaining89Zr solutions using ZR, Chelex-100, and TBP resins in the form of [89Zr]Zr-oxalate, [89Zr]Zr-chloride, and [89Zr]Zr-citrate in terms of purification and labeling efficiency. All evaluated methods allowed us to obtain89Zr with high yield (> 90% in 1 mL). The chemical form of89Zr has a significant influence on the radiolabeling efficiency of the deferoxamine (DFO) chelator and its derivatives. Compared to [89Zr]Zr-oxalate, the application of [89Zr]Zr-chloride and [89Zr]Zr-citrate solutions leads to a higher efficacy of [89Zr]Zr-DFO complex f...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 23, 2022 Category: Biochemistry Authors: Viktor Bubenshchikov,
Artur Makichyan,
Anton Larenkov Tags: RESEARCH ARTICLE Source Type: research
