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.

Peptides for trans ‐blood brain barrier delivery
Trans-blood-brain barrier (BBB) delivery of therapeutic and diagnostic agents is a major challenge in the development of central nervous system (CNS) targeted radiopharmaceuticals. This review is an introduction to the use of peptides as delivery agents to transport cargos into the CNS. The most widely used BBB penetrating peptides are reviewed here, with a particular emphasis on the broad range of cargos delivered into the CNS using these. Cell penetrating peptides (CPPs) have been deployed as trans-BBB delivery agents for some time; new developments in the CPP field offer exciting opportunities for the design of next gen...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 12, 2023 Category: Biochemistry Authors: Reuben Blades, Lars M. Ittner, Ole Tietz Tags: SPECIAL ISSUE REVIEW Source Type: research

Evaluation and improvement of CuI ‐mediated 11C‐cyanation
CuI-mediated11C-cyanation was evaluated by synthesizing [11C]perampanel and compared with previous works. In vivo evaluations of [11C]perampanel using PET imaging were performed, and it showed the rapid spreading of [11C]perampanel into the brain, heart, and lung and its accumulation in the small intestine. In addition, the reaction conditions for CuI-mediated11C-cyanation of small molecules were optimized by using K2CO3 or prolonging the reaction time, and the RCY of11C-cyanation was improved. This improved method was applied to various (hetero)aromatic bromides. CuI-mediated11C-cyanation was evaluated by synthesizing [11...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 25, 2023 Category: Biochemistry Authors: Hideki Ishii, Tomoteru Yamasaki, Toshimitsu Okamura, Yiding Zhang, Yusuke Kurihara, Masanao Ogawa, Nobuki Nengaki, Ming ‐Rong Zhang 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 - March 22, 2023 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Radioiodination, purification, and evaluation of antihuman tumor ‐derived immunoglobulin G light chain monoclonal antibody in tumor‐bearing nude mice
We report the synthesis and biological evaluation of 131I-labeled antihuman tumor-derived immunoglobulin G (IgG) light chain monoclonal antibody (4E9) ([131I]I-4E9) as a promising probe for tumor imaging. We report the synthesis and biological evaluation of131I-labeled antihuman tumor-derived immunoglobulin G (IgG) light chain monoclonal antibody (4E9) ([131I]I-4E9) as a promising probe for tumor imaging. [131I]I-4E9 was synthesized in radiochemical yield of 89.9  ± 4.7% with radiochemical purity of more than 99%. [131I]I-4E9 showed high stability in normal saline and human serum. In cell uptake studies, [131I]I-4E9 e...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 22, 2023 Category: Biochemistry Authors: Hongwei Sun, Ping Yan, Rongfu Wang, Yujing Du, Chunli Zhang, Fengqin Guo, Lei Kang, Yonggang Cui Tags: RESEARCH ARTICLE Source Type: research

Improved protocol for the radiosynthesis of [18F]FTC ‐146: A potent and selective sigma‐1 receptor radioligand
We described an optimized fully automated radiosynthesis approach afforded [18F]FTC-146 in over sevenfold higher RCYs. [18F]FTC-146 was introduced as a very potent and selective sigma-1 receptor radioligand, which has shown promising application as an imaging agent for neuropathic pain with positron emission tomography. In line with a multi-laboratory project on animal welfare, we chose this radioligand to investigate its potential for detecting neuropathic pain and tissue damage in tumor-bearing animals. However, the radiochemical yield (RCY) of around 4 –7% was not satisfactory to us, and efforts were made to improve i...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 22, 2023 Category: Biochemistry Authors: Masoud Sadeghzadeh, Barbara Wenzel, Julia Nikodemus, Alexandru Florea, Fabian Hertel, Klaus Kopka, Andreas T. J. Vogg, Fabian Kiessling, Felix M. Mottaghy 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 - March 22, 2023 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Synthesis of Beta ‐Site Amyloid Precursor Protein‐Cleaving Enzyme 1 Inhibitors BI 1147560 and BI 1181181 Labeled with Carbon‐14 and Deuterium
The generation of amyloid-beta peptides that aggregate in the brain is believed to play a major role in Alzheimer ’s disease. In theory, the inhibition of beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1), which catalyzes the initial rate-limiting step in amyloid beta production may slow or stop Alzheimer’s disease. Herein, we report the preparation of two potent BACE1 inhibitors, BI 1147560 (1) and BI 1181181 (2) labeled with carbon-14 and with deuterium. The use of advanced key chiral intermediates like 3 and 5 shortened the carbon 14 syntheses of these two compounds to five and six steps respectively and...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 18, 2023 Category: Biochemistry Authors: Bachir Latli, Matt J. Hrapchak, Jonathan T. Reeves, Heewon Lee, Jinhua J. Song Tags: RESEARCH ARTICLE Source Type: research

Radioiodination, purification, and evaluation of antihuman tumor ‐derived immunoglobulin G light chain monoclonal antibody in tumor‐bearing nude mice
We report the synthesis and biological evaluation of 131I-labeled antihuman tumor-derived immunoglobulin G (IgG) light chain monoclonal antibody (4E9) ([131I]I-4E9) as a promising probe for tumor imaging. We report the synthesis and biological evaluation of131I-labeled antihuman tumor-derived immunoglobulin G (IgG) light chain monoclonal antibody (4E9) ([131I]I-4E9) as a promising probe for tumor imaging. [131I]I-4E9 was synthesized in radiochemical yield of 89.9  ± 4.7% with radiochemical purity of more than 99%. [131I]I-4E9 showed high stability in normal saline and human serum. In cell uptake studies, [131I]I-4E9 e...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 14, 2023 Category: Biochemistry Authors: Hongwei Sun, Ping Yan, Rongfu Wang, Yujing Du, Chunli Zhang, Fengqin Guo, Lei Kang, Yonggang Cui Tags: RESEARCH ARTICLE Source Type: research

Imidazolium ‐methylene‐trifluoroborate: A novel radioprosthetic group validated with preclinical 18F‐Positron Emission Tomography imaging of Prostate Specific Membrane Antigen in mice
A new organotrifluoroborate radioprosthetic group, imidazolinium-methylene-trifluoroborate, is synthesized and appended to a ligand for aqueous one-step radiofluorination. It is validated in the context of imaging PSMA on LNCaP xenografts in mice. By slightly weakening the B-F bonds to solvolysis, radiochemical conversion by isotope exchange is increased, yet no significant bone uptake is observed in vivo, thereby validating this prosthetic for potential use in PET imaging. Organotrifluoroborates have gained acceptance as radioprosthetic groups for radiofluorination. Of these, the zwitterionic prosthetic group “AMBF3” ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 5, 2023 Category: Biochemistry Authors: Jerome Lozada, Hsiou ‐Ting Kuo, Wen Xuan Lin, Kuo‐Shyan Lin, François Bénard, David M. Perrin Tags: RESEARCH ARTICLE Source Type: research

A practical and environmentally friendly protocol for synthesis of α‐deuterated carboxylic acids
An efficient method for synthesis of α-deuterated carboxylic acids from malonic acid derivatives has been developed. Hydrogen/deuterium exchange followed by decarboxylation take place in the same vessel and resulted in high isotopic purity. α-deuterated carboxylic acids have been synthesized from the corresponding malonic acids via hydrogen/deuterium exchange and decarboxylation in presence of D2O. The method is general, mild and efficient and does not require organic solvents or other additives. Yields range between 83% and 94% and purification was not necessary. Starting materials were easy accessible and the α-deuter...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 3, 2023 Category: Biochemistry Authors: Johan Wennerberg, Klaus Dreisch Tags: RESEARCH ARTICLE Source Type: research

A practical and environmentally friendly protocol for synthesis of α‐deuterated carboxylic acids
α-deuterated carboxylic acids have been synthesised from the corresponding malonic acids via hydrogen/deuterium exchange and decarboxylation in presence of D2O. The method is general, mild and efficient and does not require organic solvents or other additives. Yields were between 83 and 94% and purification was not necessary. Starting materials were easy accessible and the α-deuterated carboxylic acids may easily be transformed to other labelled compounds such as alcohols, aldehydes, esters, amides etc. Characterization with NMR confirmed purity and isotopic purity. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 24, 2023 Category: Biochemistry Authors: Johan Wennerberg, Klaus Dreisch Tags: RESEARCH ARTICLE Source Type: research

Strategies for designing novel PET radiotracers to cross the blood brain barrier
Positron emission tomography (PET) is a powerful tool for imaging biological processes in the central nervous system (CNS). Designing PET radiotracers capable of crossing the blood-brain barrier (BBB) remains a major challenge. In addition to being brain-penetrant, a quantifiable CNS PET radiotracer must have high target affinity and selectivity, appropriate pharmacokinetics, minimal non-specific binding, negligible radiometabolites in the brain, and must be amenable to labelling with11C or18F. This review aims to give an overview of some of the critical physicochemical and biochemical contributors specific for CNS PET rad...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 23, 2023 Category: Biochemistry Authors: Anton Lindberg, Melissa Chass é, Cassis Varlow, Anna Pees, Neil Vasdev Tags: REVIEW Source Type: research