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.

Applications of radiolabeled antibodies in neuroscience and neuro ‐oncology
Application of antibodies to PET imaging of targets in the central nervous system is a particularly nascent field, but one with tremendous potential. In this review, we discuss the growth of PET in the imaging of CNS targets, present the promises and progress in antibody-based CNS PET, explore challenges faced by the field, and discuss questions that this promising approach will need to answer moving forward for imaging and perhaps even radiotherapy. Positron emission tomography (PET) is a powerful tool in medicine and drug development, allowing for non-invasive imaging and quantitation of biological processes in live orga...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - June 16, 2023 Category: Biochemistry Authors: Ryan J. Pakula, Peter J. H. Scott Tags: REVIEW Source Type: research

Development and physicochemical characterization of a biodegradable microspheres formulation loaded with samarium ‐153 and doxorubicin for chemo‐radioembolization of liver tumours
In conclusion, a novel biodegradable microspheres formulation loaded with chemotherapeutic drug (Dox) and radioactive agent (153Sm) was successfully developed in this study. The formulation fulfilled all the desired physicochemical properties of a chemo-radioembolic agent and achieved better in vitro cytotoxicity on HepG2 cells. Further investigations are needed to evaluate the biosafety, radiation dosimetry, and synergetic anticancer properties of the formulation. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - June 8, 2023 Category: Biochemistry Authors: Asseel Hisham Alregib, Hun Yee Tan, Yin How Wong, Azahari Kasbollah, Eng Hwa Wong, Basri Johan Jeet Abdullah, Alan Christopher Perkins, Chai Hong Yeong Tags: RESEARCH ARTICLE Source Type: research

Synthesis and evaluation of 111In ‐labeled tetrapeptide‐based compounds as single‐photon emission computed tomography imaging probes targeting granzyme B
In this study, we designed novel111In-labeled granzyme B-targeting single-photon emission computed tomography (SPECT) imaging probes, [111In]IDT and [111In]IDAT. Nonradioactive In-labeled granzyme B-targeting compounds ([natIn]IDT, [natIn]IDAT) showed the affinity for recombinant mouse granzyme B. [111In]IDT and [111In]IDAT were obtained with moderate radiochemical yield and high stability in mouse plasma (>95%). In a biodistribution experiment using tumor-bearing mice, [111In]IDT and [111In]IDAT showed moderate accumulation in tumor. Ex vivo autoradiography (ARG) indicated that the accumulation of radioactivity in tumo...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 30, 2023 Category: Biochemistry Authors: Nobuki Kazuta, Hiroyuki Watanabe, Masahiro Ono Tags: RESEARCH ARTICLE Source Type: research

Efficient synthesis of carbon ‐14 labeled metabolites of the strobilurin fungicide mandestrobin using biomimetic iron‐porphyrin catalyzed oxidation
Biomimetic oxidation using synthetic iron-porphyrin (F20TPPFeCl) as a catalyst eliminated a xylene moiety of the fungicide mandestrobin, uniformly labeled with carbon-14 at the benzyl ring, to produce the corresponding radiolabeled metabolite1. This reaction mechanism was investigated by identifying chemical structures of intermediate and by-products. Optimization of reaction factors based on the mechanism improved the yield of1 from mandestrobin up to 87%. Finally, various carbon-14 labeled metabolites of mandestrobin were prepared from1. Biomimetic oxidation using synthetic iron-porphyrin (F20TPPFeCl) as a catalyst elimi...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 29, 2023 Category: Biochemistry Authors: Shuichi Murata, Motohiro Kurosawa, Takuo Fujisawa Tags: RESEARCH ARTICLE Source Type: research

The inverse electron demand Diels –Alder cycloaddition with carbon‐11 and fluorine‐18: A gateway to pretargeted imaging across the blood–brain barrier
There has been increased interest in the use of inverse electron demand Diels –Alder cycloaddition reaction in pretargeted PET imaging making use of tetrazines andtrans-cyclooctenes. This has opened up the possibility to perform pretargeted PET imaging within the brain. This review highlights the development of carbon-11 and fluorine-18 radiolabelled tetrazines andtrans-cyclooctenes and then explores their ability to cross the blood –brain barrier, their stability and finally their use in pretargeted PET imaging experiments. There is increased focus on developing tools to image large biomolecules, such as antibodies, w...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 19, 2023 Category: Biochemistry Authors: Simon H. Zientek, Stephen Thompson, Selena Milicevic Sephton, Franklin I. Aigbirhio 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 - May 15, 2023 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Synthesis of BI 894416 and BI 1342561, two potent and selective spleen tyrosine kinase inhibitors, labeled with carbon 14 and with deuterium
BI 894416 andBI 1342561 are two potent and selective spleen tyrosine kinase inhibitors developed for the treatment of severe asthma. A detailed synthesis of these compounds labeled with carbon 14 and with deuterium is described. (R)-4-((R)-1-((6-(1-[tert-butyl]-1H-pyrazol-4-yl)-2-methyl-2H-pyrazolo[3,4-d]pyridin-4-yl)oxy)ethyl)pyrrolidin-2-one (BI 894416,1) and (R)-4-((R)-1-((6-(1-[tert-butyl]-1H-pyrazol-4-yl)-2,3-dimethyl-2H-indazol-4-yl)oxy)ethyl)pyrrolidin-2-one (BI 1342561,2) are two new potent and selective spleen tyrosine kinase inhibitors developed to treat severe asthma. Both compounds have similar structures and t...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 15, 2023 Category: Biochemistry Authors: Bachir Latli, Matt J. Hrapchak, Lalith P. Samankumara, Daniel R. Fandrick, Scott Pennino, Heewon Lee, Jinhua J. Song 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 - May 15, 2023 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Nitrilase mediated mild hydrolysis of a carbon ‐14 nitrile for the radiosynthesis of 4‐(7‐hydroxycarbamoyl‐[1‐14C‐heptanoyl]‐oxy)‐benzoic acid methyl ester, [14C]‐SHP‐141: A novel class I/II histone deacetylase (HDAC) inhibitor
SHP-141 (Remetinostat) is a drug candidate in Phase 1 development for the treatment of inflammatory and hyper-proliferative diseases of the skin. This drug was labelled with a single carbon-14 in four radiochemical steps and 45% yield to give[14C]-SHP-141 with a radiochemical purity of 90% and a specific activity of 190  μCi/mg. Key to the synthesis was the application of nitrilase biocatalysis, resulting in a mild and chemoselective hydrolysis. A strategy has been developed for the carbon-14 radiosynthesis of[14C]-SHP-141, a 4-(7-hydroxycarbamoyl-heptanoyloxy)-benzoic acid methyl ester derivative containing a terminal ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 15, 2023 Category: Biochemistry Authors: Sean L. Kitson, William Watters, Thomas S. Moody, Todd Chappell, Ralph Mazitschek Tags: RESEARCH ARTICLE Source Type: research

Small ‐scale two‐dimensional liquid chromatography for a preparative re‐purification of a highly labile tritium‐labeled compound
We report a case of a sensitive molecule that could not be isolated in pure form even though the chromatographic separation was successful. In this case, the use of a small-scale two-dimensional preparative liquid chromatography approach with a direct transfer interface to a second (tra pping) column resulted in a highly pure compound (>98% radiochemical purity). This approach combines high chromatographic resolution, accurate control over the re-purification process, minimal sample manipulation, and higher overall safety for the handling of radioactive samples. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 15, 2023 Category: Biochemistry Authors: Martin Sandvoss, Christian Klaus, Remo Weck, Volker Derdau, Matthias Schiell Tags: RESEARCH ARTICLE Source Type: research