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

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 20, 2022 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Good manufacturing procedure production of [18F]SynVesT ‐1, a radioligand for in vivo positron emission tomography imaging of synaptic vesicle glycoprotein 2A
A fully automated and GMP compliant synthesis of the synaptic vesicle glycoprotein 2A (SV2A) PET radioligand, [18F]SynVesT-1 was developed using a commercially available radiosynthesis module. The protocol reliably provides a pharmaceutical grade solution of [18F]SynVesT-1 suitable for clinical studies. [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 an18F-labeled SV2A PET ligand, we have developed a fully automated procedure to provide a sterile...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 10, 2022 Category: Biochemistry Authors: Kenneth Dahl, Stefan Larsson, Peter Bonn, Anita Wallin, Oleksiy Itsenko, Michael Sch öll Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research

Low ‐scale syringe‐made synthesis of 15N‐labeled oligonucleotides
A controlled pore glass (CPG)-supported oligonucleotide synthesis of DNA trinucleotide codons containing various combinations of15N-labeled nucleic bases A, G, C, and T is reported. The cost-effective protocol uses a simple commercially available equipment and an optimized amount of valuable15N-labeled phosphoramidite used for the coupling step. Fast and reasonable low-scale (200  nmol) syringe-made synthesis of15N-labeled oligonucleotides representing DNA trinucleotide codons is communicated. All codons were prepared by solid-phase controlled pore glass synthesis column technique via the phosphoramidite method. Twenty-f...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 6, 2022 Category: Biochemistry Authors: B řetislav Brož, František Tureček, Aleš Marek Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research

GMP Production of [18F]SynVesT ‐1, a Radioligand for in vivo PET Imaging of Synaptic Vesicle Glycoprotein 2A
[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. I order to fulfill the increasing clinical demand of an18F-labelled SV2A PET ligand, we have developed a fully automated procedure to provide a sterile and pyrogen –free 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 Laboratorietekni...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 1, 2022 Category: Biochemistry Authors: Kenneth Dahl, Stefan Larsson, Peter Bonn, Anita Wallin, Oleksiy Itsenko, Michael Sch öll Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research

The synthesis of deuteriated tri ‐tert‐butyl phosphine
The synthesis of deuteriated tri-tert-butyl phosphine is reported. This synthesis is an adaptation of the known procedure for tri-tert-butyl phosphinevia a Grignard intermediate. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 31, 2022 Category: Biochemistry Authors: Lucy C. Brown, Anne McGrogan, Yoan Delavoux, James M. Hogg, John D. Holbrey, H. Q. Nimal Gunaratne, Ma łgorzata Swadźba‐Kwaśny, James P. Tellam, Sarah E. Youngs Tags: SHORT NOTE Source Type: research

Low scale syringe ‐made synthesis of 15N‐labelled oligonucleotides
Fast and reasonable low-scale (200 nmol) syringe-made synthesis of15N-labelled oligonucleotides representing DNA trinucleotide codons is communicated. All codons were prepared by solid-phase controlled pore glass synthesis column technique via the phosphoramidite method. Twenty-four labelled oligonucleotides covering the DNA genetic code alphabet were prepared using commercially available reagents and affordable equipment in a reasonably short period of time, with acceptable yields and purity for direct applications in mass spectrometry. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 27, 2022 Category: Biochemistry Authors: B řetislav Brož, František Tureček, Aleš Marek Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research

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
(Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 25, 2022 Category: Biochemistry Authors: Volker Derdau, Calum Novak ‐Mitchell Tags: EDITORIAL Source Type: research