Quentin Lemesre, Augustin Malandain, Maxime Jay, David-Alexandre Buisson, Frédéric Taran, Antoine Sallustrau, Davide Audisio
{"title":"Practitioner Protocol for the Photoreduction of [14C]CO2 to [14C]CO and Its Application to the Aminocarbonylation of an Aryl Iodide","authors":"Quentin Lemesre, Augustin Malandain, Maxime Jay, David-Alexandre Buisson, Frédéric Taran, Antoine Sallustrau, Davide Audisio","doi":"10.1002/jlcr.70021","DOIUrl":"10.1002/jlcr.70021","url":null,"abstract":"<div>\u0000 \u0000 <p>Carbon-14 labeling is fundamentally important for supporting the development of new agrochemicals and pharmaceuticals. Given its critical importance, continued innovation in technologies and methodologies for radiolabeling should be strongly encouraged to better support the radiochemistry community. However, a persistent gap often exists between technological breakthroughs and their broad adoption by the scientific community. To help bridge this gap, we have developed a Practitioner Protocol detailing a recent method from our laboratory. This protocol describes how to produce <sup>14</sup>C-labeled carbon monoxide ([<sup>14</sup>C]CO) directly from the universal precursor, [<sup>14</sup>C]carbon dioxide ([<sup>14</sup>C]CO<sub>2</sub>). We hope this protocol will facilitate the adoption and implementation of this technology in other radiochemistry laboratories, thereby enhancing radiolabeling capabilities across the field.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 2","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146129751","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Synthesis of Florasulam Stable Isotopes to Enable Identification of Degradants by Mass Spectrometry for Re-registration Studies","authors":"Caroline Long, Lindsey G. Horty","doi":"10.1002/jlcr.70005","DOIUrl":"10.1002/jlcr.70005","url":null,"abstract":"<div>\u0000 \u0000 <p>Florasulam is a triazolopyrimidine herbicide that controls broadleaf and grass weeds in cereal crops and turf. It acts as an acetolactase synthase (ALS) inhibitor, blocking the synthesis of essential amino acids required for plant growth. Due to its potency, florasulam is effective at very low application rates making it cost-effective with reduced environmental off-target effects. As is common practice, florasulam has been subject to periodic reviews by regulatory agencies during re-registration requirements since its introduction into the market in 1998. The goal of these reviews is to ensure that the herbicide carries out its intended use without creating adverse side effects to humans and the environment. Since scientific methods are continually evolving and being developed, global regulatory agencies can require additional studies to address data gaps for pesticide renewals. During this re-registration process for florasulam, new environmental fate studies were conducted to meet new European Food Safety Authority (EFSA) guidelines. Consequently, florasulam-[triazole(<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>)] and florasulam-[phenyl(<sup>13</sup>C<sub>6</sub>)] stable isotopes were synthesized to support the re-registration process.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 2","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-01-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146046378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chloe C. McNamara, Agnes P. Biju, Emma Lynn M. Hipolito, Ngan T. B. Nguyen, Christopher Liang, Jogeshwar Mukherjee
{"title":"Synthesis and Evaluation of Radioiodinated [125I]7-Iodo-5H-Pyrido[4,3-B]Indole ([125I]CTAU) in Postmortem Human Alzheimer's Disease Brain","authors":"Chloe C. McNamara, Agnes P. Biju, Emma Lynn M. Hipolito, Ngan T. B. Nguyen, Christopher Liang, Jogeshwar Mukherjee","doi":"10.1002/jlcr.70003","DOIUrl":"10.1002/jlcr.70003","url":null,"abstract":"<p>The aim of this study was to further understand the tau imaging agent, flortaucipir (T807), by making small modifications and assess its effect on tau protein binding in Alzheimer's disease (<span>AD</span>). Thus, the fluoropyridyl group in T807 was replaced with an iodine atom. We report here the development and preliminary evaluation of [<sup>125</sup>I]7-iodo-5H-pyrido[4,3-B]indole ([<sup>125</sup>I]CTAU) in postmortem <span>AD</span> brain slices. Using molecular docking, binding energies of CTAU indicated weaker tau binding compared with T807. In vitro tau binding assays in <span>AD</span> brain slices measured IC<sub>50</sub> of CTAU and T807 as 44 × 10<sup>−9</sup> M and 3.8 × 10<sup>−9</sup> M, respectively. [<sup>125</sup>I]CTAU was synthesized in high radiochemical purity and molar activity (90 TBq/mmole). Binding of [<sup>125</sup>I]CTAU in the <span>AD</span> grey matter (GM) was observed, with lower nonspecific binding in the white matter (GM/WM = 2.3). Tau binding drugs (T807 and MK-6240, 10 μM) were both able to displace ~90% of bound [<sup>125</sup>I]CTAU in <span>AD</span> brain slices. Clorgyline (10 μM), a monoamine oxidase A inhibitor, decreased the binding of [<sup>125</sup>I]CTAU to 72% of total. In <span>AD</span> brain slices, [<sup>125</sup>I]CTAU exhibited a similar binding profile with the tau imaging agent [<sup>125</sup>I]IPPI. Although [<sup>125</sup>I]CTAU appears promising in vitro, any off-target issues need to be further studied to determine its use in <span>AD</span>-related dementias (ADRD).</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12789887/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145944470","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}