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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 non-alcoholic steatohepatitis (NASH). CB1 R 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 cannabinoid receptor (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 optimised [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 TFA 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 which 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 three 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
J M Coffey, A Vadas, Y Puleo, K Lewis, G Pirone, H L Rudolph, E Helms, T D Wood, A 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 (ASD), suggesting potential utility 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
O Morris, M Fairclough, J Grigg, C Prenant, A McMahon
Affinity peptide and protein- (APP) based radiotracers are an increasingly popular class of radiotracer in positron emission tomography (PET), which was once dominated by the use of small molecule radiotracers. Radiolabelled monoclonal antibodies (mAbs) are important examples of APPs yet a preference for smaller APPs, which exhibit fast pharmacokinetics and permit rapid PET aided diagnosis, has become apparent. 18 F exhibits favourable physical characteristics for APP radiolabelling and has been described as an ideal PET radionuclide...
May 8, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Ryan A Bragg, Malvika Sardana, Markus Artelsmair, Charles S Elmore
Carboxylations are an important method for the incorporation of isotopically labeled 14 CO2 into molecules. This manuscript will review labeled carboxylations since 2010 and will present a perspective on the potential of recent unlabeled methodology for labeled carboxylations. The perspective portion of the manuscript is broken into three major sections based on product type, arylcarboxylic acids, benzylcarboxylic acids, and alkyl carboxylic acids, and each of those sections is further subdivided by substrate...
May 8, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Mark H Dornan, José-Mathieu Simard, Antoine Leblond, Daniel Juneau, Guila Delouya, Fred Saad, Cynthia Ménard, Jean N DaSilva
[18 F]DCFPyL is a clinical-stage PET radiotracer used to image prostate cancer. This report details the efficient production of [18 F]DCFPyL using single-step direct radiofluorination, without the use of carboxylic acid protecting groups. Radiolabelling reaction optimization studies revealed an inverse correlation between the amount of precursor used and the radiochemical yield (RCY). This simplified approach enabled automated preparation of [18 F]DCFPyL within 28 minutes using HPLC-purification (26% ± 6%, at EOS, n = 4), which was then scaled up for large-batch production to generate 1...
May 2, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Zbigniew P Kortylewicz, Janina Baranowska-Kortylewicz
Microtubules are a target for a broad spectrum of drugs used as chemotherapeutics to treat hematological malignancies and solid tumors. Most of these drugs have significant dose-limiting toxicities including peripheral neuropathies that can be debilitating and permanent. In an ongoing effort to develop safer and more effective drugs, benzimidazole-based compounds are being developed as replacement for vincristine and similar agents. In this report, we describe radiosyntheses of novel microtubule-targeting methyl N-[5-(3'-radiohalobenzoyl)-1H-benzimidazol-2-yl]carbamates 4 that are intended as potential imaging agents and molecular radiotherapeutics...
April 29, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Volker Derdau
In this review newly developed cyanation methods are evaluated in regards to their usefulness in synthetic isotope chemistry. In combination with already established protocols in 13/14 C- or 11 C-isotope chemistry this manuscript should help isotope scientists to choose the best possible method for their scientific cyanation problem, but with the main focus on 14 C-applications. Perhaps most promising of the described novel cyanation reaction is the decarboxylation-cyanation-hydrolysis approach which makes a one-step late-stage functionalization procedure possible...
April 25, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Delphine Vivier, Sai Kiran Sharma, Brian M Zeglis
Over the past 25 years, antibodies have emerged as extraordinarily promising vectors for the delivery of radionuclides to tumors for nuclear imaging. While radioimmunoconjugates often produce very high activity concentrations in target tissues, they also are frequently characterized by elevated activity concentrations in healthy organs as well. The root of this background uptake lies in the complex network of biological interactions between the radioimmunoconjugate and the subject. In this review, we seek to provide an overview of these interactions and thus paint a general picture of the in vivo fate of radioimmunoconjugates...
April 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Futao Liu, Lin Zhu, Seok Rye Choi, Karl Plössl, Zhihao Zha, Hank F Kung
Positron emission tomography (PET) imaging of serotonin transporter (SERT) is useful for studying brain diseases with altered serotonergic function. A deuterated imaging agent, ([18 F]2-((2-((bis(methyl-d3)amino)methyl)-4-(3-fluoropropoxy- 1,1,2,2,3,3-d6)phenyl)thio)aniline, [18 F]D12FPBM, [18 F]1), was prepared as a new chemical entity (NCE). The deuterated agent, 1, showed excellent binding affinity to SERT; Ki was 0.086 nM, comparable to the un-deuterated FPBM. In vivo biodistribution studies in rats with [18 F]1 showed good brain uptake (1...
April 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Mina Jamre, Mojtaba Shamsaei, Mostafa Erfani, Sodeh Sadjadi, Mohammad Ghannadi Maragheh
Radioembolization with radioactive microspheres has been an effective method for the treatment of liver lesions. The aim of this study was to prepare carrier-free 188 Re loaded poly (L-lactic acid) (PLLA) microspheres through 188 Re sulfide colloidal nanoparticles (188 Re-SC nanoparticles). The formation of 188 Re-SC nanoparticles was confirmed by ultraviolet-visible spectrophotometry. The labeling yield of 188 Re-SC nanoparticles was verified using the RTLC method. Effects of synthesis parameters on morphology and size of prepared 188 Re-sulfide colloidal-PLLA microspheres (188 Re-SC-PLLA microspheres) were studied by scanning electron microscopy...
April 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Myoung Hyoun Kim, Seul-Gi Kim, Dae-Weung Kim
We developed a Tc-99m and TAMRA labeled peptide, Tc-99m Arginine-Arginine-Leucine (RRL) peptide (TAMRA-GHEG-ECG-RRL) to target tumor cells, and evaluated the diagnostic performance of Tc-99m TAMRA-GHEG-ECG-RRL as a dual-modality imaging agent for tumor in a murine model. TAMRA-GHEG-ECG-RRL was synthesized using Fmoc solid-phase peptide synthesis. Binding affinity and in vitro cellular uptake studies were performed. Gamma camera imaging, biodistribution and ex vivo imaging studies were performed in murine models with PC-3 tumors...
March 30, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Richard P Nugent, Crist N Filer
The synthesis of [N-methyl-3 H](+/-)-mecamylamine is described as an example of a convenient and mild method to reduce formamide groups using tritiated borane generated in situ. The product was characterized by TLC, HPLC, mass spectrometry and tritium NMR.
March 30, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Falguni Basuli, Xiang Zhang, Elaine M Jagoda, Peter L Choyke, Rolf E Swenson
Following our recently published fluorine-18 labeling method, 'Radio-fluorination on the Sep-Pak', we have successfully synthesized 6-[18 F]fluoronicotinaldehyde by passing a solution (1:4 acetonitrile: t-butanol) of its quaternary ammonium salt precursor, 6-(N,N,N-trimethylamino)nicotinaldehyde trifluoromethanesulfonate (2), through a fluorine-18 containing anion exchange cartridge (PS-HCO3 ). Over 80% radiochemical conversion was observed using 10 mg of precursor within 1 min. The [18 F]fluoronicotinaldehyde ([18 F]5) was then conjugated with 1-(6-(aminooxy)hexyl)-1H-pyrrole-2,5-dione to prepare the fluorine-18 labeled maleimide functionalized prosthetic group, 6-[18 F]fluoronicotinaldehyde O-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexyl) oxime, 6-[18 F]FPyMHO ([18 F]6)...
March 25, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Wen-Ting K Tsai, Anna M Wu
The exquisite specificity of antibodies and antibody fragments renders them excellent agents for targeted delivery of radionuclides. Radiolabeled antibodies and fragments have been successfully used for molecular imaging and radioimmunotherapy (RIT) of cell surface targets in oncology and immunology. Protein engineering has been used for antibody humanization essential for clinical applications, as well as optimization of important characteristics including pharmacokinetics, biodistribution, and clearance. Although intact antibodies have high potential as imaging and therapeutic agents, challenges include long circulation time in blood, which leads to later imaging time points post-injection and higher blood absorbed dose that may be disadvantageous for RIT...
March 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
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