Journal of Labelled Compounds and Radiopharmaceuticals 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.

Development of 11C ‐labeled CRANAD‐102 for positron emission tomography imaging of soluble Aβ‐species
CRANAD-102 is a highly promising, near-infrared fluorescence-based tracer with 68-fold selectivity for soluble oligomeric forms of amyloid β over its aggregates. This work describes the radiosynthesis of carbon-11-labeled CRANAD-102 via a Suzuki–Miyaura reaction in an RCС of 48 ± 9%, with an RCP of>96% and a molar activity of 25  ± 7 GBq/μmol. CRANAD-102, a selective near-infrared fluorescent tracer targeting soluble amyloid- β (Aβ) species, has recently attracted attention due to its potential to be used as a diagnostic tool for early stages of Alzheimer's disease (AD). Development of a positron emissio...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 1, 2023 Category: Biochemistry Authors: Markus Staudt, Vladimir Shalgunov, Maiken Nedergaard, Matthias M. Herth Tags: RESEARCH ARTICLE Source Type: research

An improved synthesis of [18F]VAT and its precursor
The synthesis method for a clinical interesting18F-labeled radiotracer, [18F]VAT, has been improved by regio- and enantio-enriched synthesis of intermediate benzovesamicol (-)5 and tosylate (-)8 as radiolabeling precursors. The simplifed radiosynthesis process features with one-step radiolabeling and much shortened production time. The vesicular acetylcholine transporter (VAChT) in the brain is an important presynaptic cholinergic biomarker, and neuroimaging studies of VAChT may provide in vivo information about psychiatric and neurologic conditions including Alzheimer's disease that are not accessible by other methods. Th...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 25, 2023 Category: Biochemistry Authors: Bao Hu, Hari K. Akula, Doyoung Noh, Yiu Fung Mui, Mark Slifstein, Ramin Parsey, Wenchao Qu Tags: RESEARCH ARTICLE Source Type: research

Automated production of 11C ‐labeled carboxylic acids and esters via “in‐loop” 11C‐carbonylation using GE FX synthesis modules
An in-loop11C-carbonylation process for the radiosynthesis of11C-carboxylic acids and esters from halide precursors is reported. The reaction proceeds at room temperature and enables11C-carbonylation of both electron deficient and electron rich (hetero)aromatic halides to provide11C-carboxylic acids and esters in good to excellent radiochemical yields, high radiochemical purity, and excellent molar activity. The process has been fully automated using commercial radiochemistry synthesis modules, and suitability for clinical production is demonstrated via validated radiosyntheses of [11C]bexarotene and [11C]acetoacetic acid....
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 23, 2023 Category: Biochemistry Authors: Tanpreet Kaur, Jay S. Wright, Bradford D. Henderson, Jonathan Godinez, Xia Shao, Peter J. H. Scott Tags: RESEARCH ARTICLE Source Type: research

Luminescence enhancement by deuterium
Deuterium, created very early in the history of the universe, has been an extraordinary discovery tool in chemistry and biology. This review describes and documents the unique influence that deuterium has often displayed on luminescence. Created literally at the dawn of time, deuterium has been extremely valuable in so many chemistry roles. The subject of this review focuses on one deuterium application in particular: its enhancement of luminescence in many substances. After providing general overviews of both deuterium and luminescence, the early exploration of deuterium's effect on luminescence is described, followed by ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 17, 2023 Category: Biochemistry Authors: Crist N. Filer Tags: REVIEW 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 - August 9, 2023 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Enzymatic synthesis of halogen derivatives of L ‐phenylalanine and phenylpyruvic acid stereoselectively labeled with hydrogen isotopes in the side chain
Halogenated, labeled with deuterium, tritium or doubly labeled with deuterium and tritium in the side chain isotopomers of L-phenylalanine and phenylpyruvic acid were synthesized. Isotopomers of halogenated L-phenylalanine were obtained by addition of ammonia to the halogenated derivative of (E)-cinnamic acid catalyzed by phenylalanine ammonia lyase (PAL). Isotopomers of halogenated phenylpyruvic acid were obtained enzymatically by conversion of the appropriate isotopomer of halogenated L-phenylalanine in the presence of PheDH. Halogenated, labeled with deuterium, tritium or doubly labeled with deuterium and tritium in the...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 8, 2023 Category: Biochemistry Authors: Katarzyna Pa łka, Katarzyna Podsadni, Małgorzata Pająk Tags: RESEARCH ARTICLE Source Type: research

Carbon 14 and stable isotope synthesis of two potent and selective phosphodiesterase type 4 inhibitors
Compounds 1 and 2 are two potent and selective inhibitors of phosphodiesterase type 4 (PDE4). In this manuscript, we report the detailed synthesis of these two compounds labeled with carbon 14, carbon 13, and deuterium. (R)-2-(4-(Benzo[d]oxazol-2-yl)piperazin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (1) and (R)-2-(4-(4-chlorophenoxy)piperidin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (2) are two potent and selective inhibitors of phosphodiesterase type 4 (PDE4). In this manuscript, we report the detailed synthesis of these two compounds ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 2, 2023 Category: Biochemistry Authors: Bachir Latli, Matt J. Hrapchak, Thomas G. Tampone, Rogelio P. Frutos, Heewon Lee Tags: RESEARCH ARTICLE Source Type: research

A practical approach to the optimization of positron emission tomography imaging agents for the central nervous system
(Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - July 21, 2023 Category: Biochemistry Tags: NOTE Source Type: research