1,937 results match your criteria radiochemical yields

A Novel Reagent for Radioiodine Labeling of New Chemical Entities (NCEs) and Biomolecules.

Molecules 2021 Jul 18;26(14). Epub 2021 Jul 18.

Laboratory for Translational Research in Imaging Pharmaceuticals, The Wright Center of Innovation in Biomedical Imaging, Department of Radiology, The Ohio State University, Columbus, OH 43212, USA.

Radioiodine labeling of peptides and proteins is routinely performed by using various oxidizing agents such as Chloramine T, Iodobeads, and Iodogen reagent and radioactive iodide (I), although some other oxidizing agents were also investigated. The main objective of the present study was to develop and test a novel reagent, inorganic monochloramine (NHCl), for radioiodine labeling of new chemical entities and biomolecules which is cost-effective, easy to make and handle, and is selective to label amino acids, peptides, and proteins. The data presented in this report demonstrate that the yields of the non-radioactive iodine labeling reactions using monochloramine are >70% for an amino acid (tyrosine) and a cyclic peptide (cyclo Arg-Gly-Asp-d-Tyr-Lys, cRGDyK). Read More

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A new approach to produce [F]MC225 via one-step synthesis, a PET radiotracer for measuring P-gp function.

EJNMMI Radiopharm Chem 2021 Jul 15;6(1):24. Epub 2021 Jul 15.

Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Centre Groningen, Hanzeplein 1, 9713, GZ, Groningen, the Netherlands.

Background: [F]MC225 is a radiotracer for imaging P-glycoprotein (P-gp) function at the blood-brain barrier. The P-gp function can be altered due to different factors, for instance, decreased P-gp function has been described in patients with Alzheimer's or Parkinson's Disease. The current applied radiosynthesis of [F]MC225 involves 2 steps, including the distillation of the [F] fluoroethylbromide intermediate. Read More

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A comparative study on Suzuki-type C-methylation of aromatic organoboranes performed in two reaction media.

J Labelled Comp Radiopharm 2021 Jul 11. Epub 2021 Jul 11.

Department of Medicinal Chemistry, Uppsala Biomedical Center, Uppsala University, Uppsala, Sweden.

The Suzuki-type cross coupling reaction is a palladium-mediated multistep reaction that has been used to synthesize several C-labeled tracers for PET. However, the impact of the selected organoborane reagent and reaction medium on the radiochemical yield (RCY) has not been thoroughly investigated. To bridge this gap, we studied the synthesis of 1-[ C]methylnaphthalene using four different organoborane precursors in reactions performed in DMF/water and THF/water. Read More

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Development and in vitro evaluation of new bifunctional Zr-chelators based on the 6-amino-1,4-diazepane scaffold for immuno-PET applications.

Nucl Med Biol 2021 Jun 29;102-103:12-23. Epub 2021 Jun 29.

Department of Chemistry - TRIGA site, Johannes Gutenberg University Mainz, Germany. Electronic address:

Introduction: Combination of hydroxamate bearing side chains with the 6-amino-1,4-diazepane scaffold provides a promising strategy for fast and stable Zr-labeling of antibodies. Following this approach, we hereby present the development, labeling kinetics and in vitro complex stability of three resulting bifunctional chelator derivatives both stand-alone and coupled to a model protein in comparison to different linear deferoxamine (DFO) derivatives.

Methods: The novel Zr-chelator HyADA was prepared via amide-coupling of separately synthesized 6-amino-1,4-diazepane-6-pentanoic acid and hydroxamate-containing side chains. Read More

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Automated production of [F]Flortaucipir for PET imaging of tauopathies.

Am J Nucl Med Mol Imaging 2021 15;11(3):167-177. Epub 2021 Jun 15.

Department of Radiology, Mayo Clinic Jacksonville, FL, USA.

Radiotracer [F]Flortaucipir is an FDA-approved diagnostic agent for PET imaging of density and distribution of abnormal tau protein deposition (tauopathies) in Alzheimer's disease. A high-yield automated method for routine GMP-compliant [F]Flortaucipir production is desired to meet increasing clinical need. In this work, we reported an automated radiosynthesis of [F]Flortaucipir in a RNplus Research module and the quality control (QC) tests for human use under full GMP compliance. Read More

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Noninvasively visualize the expression of LAPTM4B protein using a novel F-labeled peptide PET probe in hepatocellular carcinoma.

Nucl Med Biol 2021 Jun 19;100-101:52-60. Epub 2021 Jun 19.

Nanfang PET Center, Nanfang Hospital, Southern Medical University, Guangzhou, China. Electronic address:

Objective: Lysosomal protein transmembrane 4 beta (LAPTM4B) is selectively expressed in hepatocellular carcinoma (HCC) cells and thus a potential biomarker for diagnosing HCC. In this study, we designed a novel F-labeled PET probe to non-invasively visualize LAPTM4B expression in mouse model of HCC tumor.

Methods: A PET targeting tracer named [F]FP-LAP2H was radio-synthesized using a LAPTM4B targeting peptide, LAP2H, coupled with 4-nitrophenyl-2-[F]fluoropropionate ([F]NFP). Read More

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Development of Radiofluorinated Nicotinamide/Picolinamide Derivatives as Diagnostic Probes for the Detection of Melanoma.

Int J Mol Sci 2021 Jun 16;22(12). Epub 2021 Jun 16.

Department of Biomedical Imaging and Radiological Sciences, National Yang Ming Chiao Tung University, Taipei 112, Taiwan.

Regarding the increased incidence and high mortality rate of malignant melanoma, practical early-detection methods are essential to improve patients' clinical outcomes. In this study, we successfully prepared novel picolinamide-benzamide (F-FPABZA) and nicotinamide-benzamide (F-FNABZA) conjugates and determined their biological characteristics. The radiochemical yields of F-FPABZA and F-FNABZA were 26 ± 5% and 1 ± 0. Read More

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Introduction of Re(CO)/Tc(CO) Organometallic Species into Vinylpyrrolidone-Allyliminodiacetate Copolymers.

Polymers (Basel) 2021 Jun 1;13(11). Epub 2021 Jun 1.

Federal State Budgetary Institution of Science Institute of Macromolecular Compounds, Russian Academy of Sciences (IMC RAS), Russian Federation, V.O. Bolshoy pr. 31, 199004 Saint Petersburg, Russia.

N-vinylpyrrolidone-co-allylamine copolymers (VP-co-AA) containing iminodiacetic (IDA) chelation units were prepared in the range of molecular masses of the copolymers from 9000 to 30,000 Da depending on polymerization conditions. Non-radioactive organometallic species Re(CO) were introduced into polymeric carriers under mild conditions; the prepared metal-polymeric complexes were characterized by IR, NMR, ESI-MS and HPLC. IR spectra data confirmed the coordination of M(CO) moiety to the polymeric backbone via IDA chelation unit (appearance of characteristic fac-M(CO) vibrations (2005, 1890 cm), as well as the appearance of group of signals in H NMR spectra, corresponding to those inequivalent to methylene protons CHCOO (dd, 4. Read More

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Design, Synthesis, In Vitro and In Vivo Evaluation of Heterobivalent SiFA-Modified Peptidic Radioligands Targeting Both Integrin αβ and the MC1 Receptor-Suitable for the Specific Visualization of Melanomas?

Pharmaceuticals (Basel) 2021 Jun 7;14(6). Epub 2021 Jun 7.

Molecular Imaging and Radiochemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany.

Combining two peptides addressing two different receptors to a heterobivalent peptidic ligand (HBPL) is thought to enable an improved tumor-targeting sensitivity and thus tumor visualization, compared to monovalent peptide ligands. In the case of melanoma, the Melanocortin-1 receptor (MC1R), which is stably overexpressed in the majority of primary malignant melanomas, and integrin αβ, which is involved in lymph node metastasis and therefore has an important role in the transition from local to metastatic disease, are important target receptors. Thus, if a radiolabeled HBPL could be developed that was able to bind to both receptor types, the early diagnosis and correct staging of the disease would be significantly increased. Read More

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Geant4-DNA simulation of the pre-chemical stage of water radiolysis and its impact on initial radiochemical yields.

Phys Med 2021 Jun 28;88:86-90. Epub 2021 Jun 28.

UMR 5797, Bordeaux University, CNRS, CENBG, 33170 Gradignan, France.

This paper demonstrates the impact of the pre-chemical stage, especially the dissociation scheme and the associated probabilities, on water radiolysis simulation using the Geant4-DNA Monte Carlo track structure simulation toolkit. The models and parameters provided by TRACs have been collected and implemented into Geant4-DNA. In order to evaluate their influence on water radiolysis simulation, the radiochemical yields (G-values) are evaluated as a function of time and LET using the "chem6" Geant4-DNA example, and they are compared with published experimental and calculated data. Read More

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Clickable Radiocomplexes With Trivalent Radiometals for Cancer Theranostics: and Studies.

Front Med (Lausanne) 2021 11;8:647379. Epub 2021 Jun 11.

Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Campus Tecnológico e Nuclear, Lisbon, Portugal.

Pre-targeting approaches based on the inverse-electron-demand Diels-Alder (iEDDA) reaction between strained trans-cyclooctenes (TCO) and electron-deficient tetrazines (Tz) have emerged in recent years as valid alternatives to classic targeted strategies to improve the diagnostic and therapeutic properties of radioactive probes. To explore these pre-targeting strategies based on click chemistry, a small family of clickable chelators was synthesized and radiolabelled with medically relevant trivalent radiometals. The structure of the clickable chelators was diversified to modulate the pharmacokinetics of the resulting [In]In-radiocomplexes, as assessed upon injection in healthy mice. Read More

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Aliphatic 18F-Radiofluorination - Recent Advances in the Labeling of Base-Sensitive Substrates.

ChemMedChem 2021 Jun 24. Epub 2021 Jun 24.

Kobenhavns Universitet, Department of Durg Design and Pharmacology, Jagtvej 160, 2100, Copenhagen, DENMARK.

Aliphatic fluorine-18 radiolabeling is the most commonly used method to synthesize tracers for PET-imaging. With an increasing demand for 18 F-radiotracers for clinical applications, new labeling strategies aiming to increase radiochemical yields of established tracers or more importantly to enable 18 F-labeling of new scaffolds have been developed. In recent years, increased attention has been focused on the direct aliphatic 18 F-fluorination of base-sensitive substrates in this respect. Read More

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Investigation on the reactivity of nucleophilic radiohalogens with arylboronic acids in water: access to an efficient single-step method for the radioiodination and astatination of antibodies.

Chem Sci 2020 Nov 23;12(4):1458-1468. Epub 2020 Nov 23.

Université de Nantes, CNRS, Inserm, CRCINA F-44000 Nantes France

Easy access to radioiodinated and At-labelled bio(macro)molecules is essential to develop new strategies in nuclear imaging and targeted radionuclide therapy of cancers. Yet, the labelling of complex molecules with heavy radiohalogens is often poorly effective due to the multiple steps and intermediate purifications needed. Herein, we investigate the potential of arylboron chemistry as an alternative approach for the late stage labelling of antibodies. Read More

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November 2020

Synthesis of [At]4-astato-L-phenylalanine by dihydroxyboryl-astatine substitution reaction in aqueous solution.

Sci Rep 2021 Jun 21;11(1):12982. Epub 2021 Jun 21.

Institute for Radiation Sciences, Osaka University, Suita, 565-0871, Japan.

Astatine-211 (At)-labeled phenylalanine is expected to be a promising agent for targeted alpha-particle therapy for the treatment of patients with glioma. The existing reactions to prepare the labeled compound usually require organic solvents and metals that are toxic and hazardous to the environment. In this study, we developed a novel method wherein astatination was realized via the substitution of At for a dihydroxyboryl group coupled to phenylalanine. Read More

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Labeling single domain antibody fragments with F using a novel residualizing prosthetic agent - N-succinimidyl 3-(1-(2-(2-(2-(2-[F]fluoroethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)-5-(guanidinomethyl)benzoate.

Nucl Med Biol 2021 Jun 11;100-101:24-35. Epub 2021 Jun 11.

Department of Radiology, Duke University Medical Center, Durham, NC, USA. Electronic address:

Introduction: Labeling single domain antibody fragments (sdAbs) with F is an attractive strategy for immunoPET. Earlier, we developed a residualizing label, N-succinimidyl 3-((4-(4-fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(guanidinomethyl)benzoate ([F]RL-I), synthesized via a click reaction for labeling sdAbs with F, that has attractive features but suffered from modest radiochemical yields and suboptimal hydrophobicity. Herein, we have evaluated the potential utility of an analogous agent, N-succinimidyl 3-(1-(2-(2-(2-(2-[F]fluoroethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)-5-(guanidinomethyl)benzoate ([F]SFETGMB; [F]RL-III) designed to address these limitations. Read More

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Transition-metal-free nucleophilic At-astatination of spirocyclic aryliodonium ylides.

Org Biomol Chem 2021 Jun;19(25):5525-5528

Faculty of Pharmaceutical Science, Hokkaido University, Sapporo 060-0812, Japan. and Global Station for Biosurfaces and Drug Discovery, Hokkaido University, Sapporo 060-0812, Japan.

The transition-metal-free 211At-astatination of spirocyclic aryliodonium ylides via a nucleophilic aromatic substitution reaction is described. This method enables the preparation of 211At-radiolabeled compounds derived from multi-functionalized molecules and heteroarenes in good to excellent radiochemical yields. Read More

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GMP production of 6-[F]Fluoro-L-DOPA for PET/CT imaging by different synthetic routes: a three center experience.

EJNMMI Radiopharm Chem 2021 Jun 12;6(1):21. Epub 2021 Jun 12.

Department of Nuclear Medicine, Copenhagen University Hospital Herlev and Gentofte, Borgmester Ib Juuls vej 31, DK-2730, Herlev, Denmark.

Background: The radiofluorinated levodopa analogue 6-[F]F-L-DOPA (3,4-dihydroxy-6-F-L-phenylalanine) is a commonly employed radiotracer for PET/CT imaging of multiple oncological and neurological indications. An unusually large number of different radiosyntheses have been published to the point where two different Ph. Eur. Read More

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Metabolic radiolabeling and in vivo PET imaging of cytotoxic T lymphocytes to guide combination adoptive cell transfer cancer therapy.

J Nanobiotechnology 2021 Jun 10;19(1):175. Epub 2021 Jun 10.

Medical Isotopes Research Center and Department of Radiation Medicine, School of Basic Medical Sciences, Peking University Health Science Center, Beijing, 100191, China.

Background: Adoptive T cell transfer-based immunotherapy yields unsatisfactory results in the treatment of solid tumors, partially owing to limited tumor infiltration and the immunosuppressive microenvironment in solid tumors. Therefore, strategies for the noninvasive tracking of adoptive T cells are critical for monitoring tumor infiltration and for guiding the development of novel combination therapies.

Methods: We developed a radiolabeling method for cytotoxic T lymphocytes (CTLs) that comprises metabolically labeling the cell surface glycans with azidosugars and then covalently conjugating them with Cu-1,4,7-triazacyclononanetriacetic acid-dibenzo-cyclooctyne (Cu-NOTA-DBCO) using bioorthogonal chemistry. Read More

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[Long-term Quality Control Test of a Ge/Ga Generator].

Kaku Igaku 2021 ;58(1):47-58

Central Institute of Isotope Science, Hokkaido University.

Quality of the Ga solution eluted from a Ge/Ga generator (Galli Eo) was evaluated. Elution was performed 488 times from 21 to 484 days (ca. 15 months) after the calibration date. Read More

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January 2021

Tuning the Kinetic Inertness of Bi Complexes: The Impact of Donor Atoms on Diaza-18-Crown-6 Ligands as Chelators for Bi Targeted Alpha Therapy.

Inorg Chem 2021 Jun 8;60(12):9199-9211. Epub 2021 Jun 8.

Department of Chemistry and Chemical Biology, Cornell University, Ithaca, New York 14853, United States.

The radionuclide Bi can be applied for targeted α therapy (TAT): a type of nuclear medicine that harnesses α particles to eradicate cancer cells. To use this radionuclide for this application, a bifunctional chelator (BFC) is needed to attach it to a biological targeting vector that can deliver it selectively to cancer cells. Here, we investigated six macrocyclic ligands as potential BFCs, fully characterizing the Bi complexes by NMR spectroscopy, mass spectrometry, and elemental analysis. Read More

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Development and evaluation of [F]Flotaza for Aβ plaque imaging in postmortem human Alzheimer's disease brain.

Bioorg Med Chem Lett 2021 Aug 1;46:128164. Epub 2021 Jun 1.

Preclinical Imaging, Department of Radiological Sciences, University of California, Irvine 92697, USA. Electronic address:

Positron emission tomographic (PET) studies of amyloid β (Aβ) accumulation in Alzheimer's disease (AD) have shown clinical utility. The aim of this study was to develop and evaluate the effectiveness of a new fluorine-18 radiotracer [F]Flotaza (2-{2-[2-[F]fluoroethoxy]ethoxy}ethoxy)-4'-N,N-dimethylaminoazobenzene), for Aβ plaque imaging. Nucleophilic [F]fluoride was used in a one-step radiosynthesis for [F]flotaza. Read More

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Radiosynthesis and Biological Evaluation of [F]R91150, a Selective 5-HT Receptor Antagonist for PET-Imaging.

ACS Med Chem Lett 2021 May 1;12(5):738-744. Epub 2021 Apr 1.

Forschungszentrum Jülich GmbH, Institute of Neuroscience and Medicine, INM-5, Nuclear Chemistry (INM-5), 52425 Jülich, Germany.

Serotonergic 5-HT receptors in cortical and forebrain regions are an important substrate for the neuromodulatory actions of serotonin in the brain. They have been implicated in the etiology of many neuropsychiatric disorders and serve as a target for antipsychotic, antidepressant, and anxiolytic drugs. Positron emission tomography imaging using suitable radioligands can be applied for quantification of receptor densities and receptor occupancy for therapy evaluation. Read More

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Detailed Chemistry Studies of 225Actinium Labeled Radiopharmaceuticals.

Curr Radiopharm 2021 May 28. Epub 2021 May 28.

Moltek A. S. Gebze Organize Sanayi, 41400 Gebze, Kocaeli, Turkey.

Background: Synthesis of 225Actinium derivatives using PSMA-617, DOTATATE peptides and EDTMP ligand was afforded. Detailed experimental, quality control (QC) and stability studies were well described. The radiolabelling reactions were performed in mild conditions with desirable radiochemical yields and high radiochemical purities. Read More

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Optimised GMP-compliant production of [F]DPA-714 on the Trasis AllinOne module.

EJNMMI Radiopharm Chem 2021 May 26;6(1):20. Epub 2021 May 26.

Department of Radiology and Nuclear Medicine, Radboud University Medical Center, Geert Grooteplein 10, Nijmegen, 6525 GA, Netherlands.

Background: The translocator protein 18 kDa is recognised as an important biomarker for neuroinflammation due to its soaring expression in microglia. This process is common for various neurological disorders. DPA-714 is a potent TSPO-specific ligand which found its use in Positron Emission Tomography following substitution of fluorine-19 with fluorine-18, a positron-emitting radionuclide. Read More

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F-Labeled magnetic nanovectors for bimodal cellular imaging.

Biomater Sci 2021 Jul 25;9(13):4717-4727. Epub 2021 May 25.

Institute of Inorganic Chemistry, University of Cologne, D-50939 Cologne, Germany.

Surface modification of nanocarriers enables selective attachment to specific molecular targets within a complex biological environment. Besides the enhanced uptake due to specific interactions, the surface ligands can be utilized for radiolabeling applications for bimodal imaging ensured by positron emission topography (PET) and magnetic resonance imaging (MRI) functions in one source. Herein, we describe the surface functionalization of magnetite (FeO) with folic acid as a target vector. Read More

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Fluorine-18 labelled Ruppert-Prakash reagent ([F]MeSiCF) for the synthesis of F-trifluoromethylated compounds.

Chem Commun (Camb) 2021 May;57(43):5286-5289

Amsterdam UMC, VU University, Radiology and Nuclear medicine, Radionuclide Center, De Boelelaan 1085c, Amsterdam, The Netherlands.

This article describes the first synthesis and application of fluorine-18 labelled Ruppert-Prakash reagent [18F]Me3SiCF3. [18F]Me3SiCF3 was synthesized from [18F]fluoroform with radiochemical yields of 85-95% and radiochemical purities of >95% within 20 minutes. 18F-trifluoromethylated compounds were successfully prepared by reaction of [18F]Me3SiCF3 with benzaldehydes, acetophenones and benzophenones. Read More

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Direct F-Labeling of Biomolecules via Spontaneous Site-Specific Nucleophilic Substitution by F on Phosphonate Prostheses.

Org Lett 2021 Jun 4;23(11):4261-4266. Epub 2021 May 4.

Centre for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, Fujian 361102, P.R. China.

We describe a high radiochemical yield late-stage direct F-labeling of bare biomolecules containing common active groups. Spontaneity and site-selectivity are attributed to the remarkably higher rates of nucleophilic substitution reactions on phosphonates than on other electrophiles by F at various hydrogen bond forms. Rapid access to many medicinally significant F-labeled biomolecules is achieved at 21-68% radiochemical yields and 35. Read More

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New Bioconjugated Technetium and Rhenium Folates Synthesized by Transmetallation Reaction with Zinc Derivatives.

Molecules 2021 Apr 19;26(8). Epub 2021 Apr 19.

Unitat de Biofísica/Centre d'Estudis en Biofísica, Facultat de Medicina, Departament de Bioquímica i Biologia Molecular, Universitat Autònoma de Barcelona, 08193 Cerdanyola del Vallès, Catalonia, Spain.

The zinc dithiocarbamates functionalized with folic acid and were synthesized with a simple straightforward method, using an appropriated folic acid derivative and a functionalized zinc dithiocarbamate (). Zinc complexes and show very low solubilities in water, making them useful for preparing Tc-99m radiopharmaceuticals with a potentially high molar activity. Thus, the transmetallation reaction in water medium between the zinc complexes or and the cation -[Tc(HO)(CO)], in the presence of the monodentate ligand TPPTS, leads to the formation of the 2 + 1 complexes -[Tc(CO)(SS)(P)] bioconjugated to folic acid ( and ). Read More

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Synthesis and Evaluation of Novel Norfloxacin Isonitrile Tc Complexes as Potential Bacterial Infection Imaging Agents.

Pharmaceutics 2021 Apr 9;13(4). Epub 2021 Apr 9.

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.

To develop potential technetium-99m single-photon emission computed tomography (SPECT) imaging agents for bacterial infection imaging, the novel norfloxacin isonitrile derivatives CN4NF and CN5NF were synthesized and radiolabeled with a [Tc][Tc(I)] core to obtain [Tc]Tc-CN4NF and [Tc]Tc-CN5NF. These compounds were produced in high radiolabeling yields and showed hydrophilicity and good stability in vitro. The bacterial binding assay indicated that [Tc]Tc-CN4NF and [Tc]Tc-CN5NF were specific to bacteria. Read More

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Preparation and Preliminary Evaluation of Neurotensin Radiolabelled with Ga and Lu as Potential Theranostic Agent for Colon Cancer.

Pharmaceutics 2021 Apr 7;13(4). Epub 2021 Apr 7.

Radiopharmaceutical Research Centre, Horia Hulubei National Institute for Physics and Nuclear Engineering, 30 Reactorului Street, Măgurele, 077125 Ilfov, Romania.

The neurotensin is a tridecapeptide involved in the proliferation of colon cancer, the overexpression of neurotensin receptors occurring at an early stage development of many tumours. Targeting neurotensin receptors by using the same biological active molecule is an effective approach for both imaging quantification and treatment. The present work aimed to demonstrate the ability of radiolabelled neurotensin to specifically target colon cancer cells, and substantiate its usefulness in targeted imaging and radiotherapy, depending on the emission of the coupled radioisotope. Read More

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