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Journal of Labelled Compounds & Radiopharmaceuticals

Crist N Filer, Demetri Orphanos
The two step synthesis of [1-14 C]tyramine hydrochloride is described with the product being characterized by TLC, HPLC and UV spectroscopy. Several methods are provided to purify [1-14 C]tyramine hydrochloride and its storage and stability are also discussed.
July 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Lu Chen, Yong Gong, Rhys Salter
Ketamine is a well-known general anesthetic that inhibits cerebral NMDA receptors. Norketamine is a major circulating metabolite of this drug. A nasal spray formulation of esketamine, the S enantiomer of ketamine is under development for the management of treatment resistant depression. In order to assess the pharmacokinetic properties, C-14 labeled ketamine and norketamine were prepared separately from commercially available [14 C]CuCN through a five-step sequence with the C-14 label at the quaternary carbon of the cyclohexyl ring...
July 10, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Masafumi Tanaka, Akira Hosotani, Takahiro Mukai
Discoidal lipid nanoparticles mimicking native high-density lipoproteins (HDL) are promising delivery vehicles of drugs and/or imaging agents. However, little is known about the in vivo biodistribution of such discoidal lipid nanoparticles compared to liposomes, clinically available spherical lipid nanoparticles. Recently, it has been reported that synthetic polymers instead of apolipoproteins can be complexed with phospholipid to form discoidal nanoparticles. In the present study, with the aim of developing phospholipid-synthetic polymer complexes for future clinical applications, the biodistribution of such particles in normal mice was investigated...
July 4, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Antonio Del Vecchio, Gianluca Destro, Frédéric Taran, Davide Audisio
Heterocycles play an essential role in modern pharmaceutical and agrochemical developments, representing a very common structural unit in marketed drugs. Over the 46 new drugs approved in 2017 by the FDA, 25 contain in their structure an heterocyclic core. The development of novel and straightforward labeling strategies for the effective insertion of carbon isotopes into heterocylic scaffolds is an inspiring and vibrant field of research. The use of carbon-11, carbon-13 and carbon-14 isotopes is well established in life science and particularly in pharmaceutical and agrochemical industry...
June 20, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Bo Zhang, Giancarlo Pascali, Naomi Wyatt, Lidia Matesic, Mitchell A Klenner, Tiffany R Sia, Adam J Guastella, Massimiliano Massi, Andrea J Robinson, Benjamin H Fraser
Fluorine-18 labelled prosthetic groups (PGs) are often necessary for radiolabelling sensitive biological molecules such as peptides and proteins. Several shortcomings, however, often diminish the final yield of radiotracer. In an attempt to provide higher yielding and operationally efficient tools for radiolabelling biological molecules, we describe herein the first radiochemical synthesis of [18 F] ethenesulfonylfluoride ([18 F] ESF) and its Michael conjugation with amino acids and proteins. The synthesis of [18 F] ESF was optimised using a microfluidic reactor under both carrier-added (c...
June 20, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Xiaoxi Pang, Meng Liu, Rongfu Wang, Xuhe Liao, Ping Yan, Chunli Zhang
The overall aim of this study was to evaluate whether iodine-131 radiolabeled monoclonal antibody (mAb) targeting PD-L1 can be used for imaging of PD-L1 expression noninvasively in vivo, and playing synergistic effect combined with immunotherapy. Anti-PD-L1 mAb was radiolabeled with iodine-131 (131 I-PD-L1 mAb), and was characterized in vitro. Biodistribution and imaging in vivo were performed periodically. Therapy study was conducted in triple-negative breast cancer bearing BALB/c mice. As results, the labeling efficiencies of 131 I-PD-L1 mAb reached 80 % ± 3 %, with radiochemical purity was 97 % ± 1 %...
June 20, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Chandan Kumar, Rohit Sharma, Tapas Das, Aruna Korde, H D Sarma, Sharmila Banerjee, Ashutosh Dash
Bone pain is the major manifestations of skeletal metastases. Although various treatment modalities are available for bone pain palliation, use of radiolabeled phosphonates is documented to be more effective. Among radionuclides available for this purpose, lutetium-177 is gaining popularity due to its moderate beta energy, theranostic capability, favorable half-life and convenient production logistics. 177 Lu-DOTMP has shown considerable promise as a metastatic bone pain palliating agent in preliminary evaluations and recent clinical studies...
June 20, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Patrik Nordeman, Ulrika Yngve, Helena Wilking, Sven Åke Gustavsson, Jonas Eriksson, Gunnar Antoni
The radiosynthesis and GMP validation of [11 C] AMT for human use is described. Three consecutive batches were produced giving 940-3790 MBq (4-17% RCY, decay corrected, based on [11 C]CO2 ). The molar activity at the end of synthesis was 19-35 GBq/μmol, the radiochemical purity was ≥98% and the enantiomeric purity was >99%. While the synthesis method was automated using a new generation of synthesis equipment, Tracer Production System (TPS) developed in house, the method should be readily applicable to other synthesis platforms with minor modifications...
June 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Allison K Zarkin, Phyllis D Elkins, Amanda Gilbert, Teresa L Jester, Herbert H Seltzman
5-Aminoimidazole-4-carboxamide-1-β-D-[13 C5 ] ribofuranosyl 5'-monophosphate ([13 C5 ribose] AICAR-PO3 H2 ) (6) has been synthesized from [13 C5 ]adenosine. Incorporation of the mass-label into [13 C5 ribose] AICAR-PO3 H2 provides a useful standard to aid in metabolite identification and quantification in monitoring metabolic pathways. A synthetic route to the 13 C-labeled compound has not been previously reported. Our method employs a hybrid enzymatic and chemical synthesis approach that applies an enzymatic conversion from adenosine to inosine followed by a ring-cleavage of the protected inosine...
June 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Zheng-Min Yang, Ya-Jun Xu, Gui-Hua Zhang, Cai-Guang Jian, Li Xiao, Qing-Fu Ye
ZJ0712, a broad-spectrum fungicidal ingredient of strobilurin, exhibits a high protective and curative activity against plant pathogenic fungi. To support the study on its metabolism, residue, environmental behavior and fate for safety evaluation, two versions of carbon-14 labelled ZJ0712, methyl (E)-2-(2-((2,5-dimethylphenoxy)methyl)phenyl)-3-methoxy[2-14 C] acrylate (2) and methyl (E)-2-(2-((2,5-dimethyl [phenyl-U-14 C6 ]phenoxy)methyl)phenyl)-3-methoxyacrylate (3), were synthesized from barium [14 C] carbonate in six-step yield of 47% and from 2,5-dimethyl [phenyl-U-14 C6 ] phenol in the yield of 91%, respectively...
June 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Dennis U Nielsen, Karoline T Neumann, Anders T Lindhardt, Troels Skrydstrup
Carbon monoxide represents the most important C1-building block for the chemical industry, both for the production of bulk and fine chemicals, but also for synthetic fuels. Yet its toxicity and subsequently its cautious handling have limited its applications in medicinal chemistry research and in particular for the synthesis of pharmaceutically relevant molecules. Recent years have nevertheless witnessed a considerable headway on the development of carbon monoxide surrogates and reactor systems, which provide an ideal setting for performing carbonylation chemistry with stoichiometric and substoichiometric carbon monoxide...
June 1, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Kuo Gai, Yu Huang, Baomin Liu, Yinsheng Zhang
Simple and facile methods for the synthesis of deuterium-labeled obeticholic acid and its 2 metabolites, glycine and taurine conjugates of obeticholic acid, are described herein. The 3 deuterated compounds were applicable for use as internal standards in drug development.
May 29, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Mohammad Amin Ahmadi Faghih, Mohammad Hossein Moslemin, Gholamhossein Shirvani, Mohsen Javaheri
The importance of DHPs compounds and the need for examining the mechanism of their effect, mandated us to synthesize a number of carbon-14 labeled 1,4-dihydropyridine derivatives for pharmacological studies. Simple preparation and suitable radiochemical yield were advantages of this preparation.
May 23, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Malliga R Iyer, Resat Cinar, Nathan J Coffey, George Kunos
Cannabinoid-1 receptor (CB1 R) antagonists/inverse agonists have great potential in the treatment of metabolic disorders like dyslipidemia, type 2 diabetes, and nonalcoholic steatohepatitis. Cannabinoid-1 receptor inverse agonists have also been reported to be effective in mitigating fibrotic disorders in murine models. Inducible nitric oxide synthase is another promising target implicated in fibrotic and inflammatory disorders. We have disclosed MRI-1867 as a potent and selective, peripherally acting dual-target inhibitor of the CB1 R and inducible nitric oxide synthase (iNOS)...
May 23, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Karin M Nielsen, Nis P Jørgensen, Majbritt H Kyneb, Per Borghammer, Rikke L Meyer, Trine R Thomsen, Dirk Bender, Svend B Jensen, Ole L Nielsen, Aage K O Alstrup
The development of bacteria-specific infection radiotracers is of considerable interest to improve diagnostic accuracy and enabling therapy monitoring. The aim of this study was to determine if the previously reported radiolabelled 1,4,7,10-tetraazacyclododecane-N,N',N″,N‴-tetraacetic acid (DOTA) conjugated peptide [68 Ga]Ga-DOTA-K-A9 could detect a staphylococcal infection in vivo and distinguish it from aseptic inflammation. An optimized [68 Ga]Ga-DOTA-K-A9 synthesis omitting the use of acetone was developed, yielding 93 ± 0...
May 23, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Dieter Muri, Martin R Edelmann
This practitioner protocol describes the use and application of different types of solid-phase extractions and metal scavengers for small-scale reactions, particularly in the context of purifying tritiated molecules from heavily contaminated reaction mixtures. Polymer-bound strong cation exchangers are especially suitable for separating basic compounds from neutral or acidic molecules and have been widely applied in the work-up of iridium-based hydrogen isotope exchange reactions. Polymer-bound strong anion exchangers can help to separate acidic compounds from their neutral or basic counterparts or to easily convert a trifluoroacetate or formate salt to its free base after HPLC purification...
May 19, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Jason P Holland
No abstract text is available yet for this article.
May 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Baomin Liu, Hui Qin, Yinsheng Zhang
Bendamustine hydrochloride is an alkylating agent that was developed for the treatment of various human cancers. The stable isotope-labeled bendamustine was required to support clinic studies. An effective and operationally simple method for the synthesis of [D6 ] bendamustine hydrochloride was developed using DCl as a catalyst and D2 O as a deuterium source. Under the present condition, regioselectively deuterated bendamustine hydrochloride with high deuterium incorporation is achieved.
May 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Bachir Latli, Matt Hrapchak, Maxim Cheveliakov, Jonathan T Reeves, Maurice Marsini, Carl A Busacca, Chris H Senanayake
1-(4-Fluorophenyl)-1H-pyrazolo[3,4-c]pyridine-4-carboxylic acid (2-methanesulfonyl-pyridin-4-ylmethyl)-amide (1) and its analogs (2) and (3) are potent CCR1 antagonists intended for the treatment of rheumatoid arthritis. The detailed syntheses of these 3 compounds labeled with carbon-13 as well as the preparation of (1) and (2) labeled with carbon-14, and (1) labeled with tritium, are described.
May 15, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Jordan M Coffey, Andrew J Vadas, Thomas R Puleo, Katelyn P Lewis, Gregory F Pirrone, Heather L Rudolph, Eric D Helms, Troy D Wood, Amber Flynn-Charlebois
Stercobilin is an end-stage metabolite of hemoglobin, a component of red blood cells. It has been found that there is a significantly lower concentration of stercobilin in the urine of people diagnosed with autism spectrum disorders, suggesting potential use as a biomarker. In vitro, we have synthesized stercobilin from its precursor bilirubin through a reduction reaction proceeded by an oxidation reaction. In addition, we have isotopically labeled the stercobilin product with deuterium using this protocol...
May 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
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