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Journal of Labelled Compounds & Radiopharmaceuticals

Koki Hasegawa, Emi Kawachi, Yoshinari Uehara, Tsuyoshi Yoshida, Satoshi Imaizumi, Masahiro Ogawa, Shin-Ichiro Miura, Keijiro Saku
We examined the (68) Ga labeling of the α-helical peptide, DOTA-FAMP, and evaluated conformational changes during radiolabeling. (68) Ga-DOTA-FAMP is a positron emission tomography probe candidate for atherosclerotic plaques. The labeling yield achieved by Zhernosekov's method (using acetone for (68) Ga purification) was compared with that achieved by the original and 2 modified Mueller's methods (using NaCl solution). Modified method I involves desalting the (68) Ga prior to labeling, and modified method II involves the inclusion of ethanol in the labeling solution...
December 7, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Sankha Chattopadhyay, Md Neyar Alam, Madhu Smita, Umesh Kumar, Sujata Saha Das, Luna Barua
Gallium-68 radioisotope is an excellent source in clinical positron emission tomography application due to its ease of availability from germanium-68 ((68) Ge)/gallium-68 ((68) Ga) generator having a shelf life of 1 year. In this paper, a modified method for purification of the primary eluate of (68) Ge-(68) Ga generator by using a small cation exchange resin (Dowex-50) column has been described. The breakthrough of (68) Ge before and after purification of (68) Ga eluate was 0.014% and 0.00027%, respectively...
December 1, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Boris A Czeskis, Darlene K Satonin
The synthesis of the radiolabeled glucagon receptor antagonist 1-[(14) C] was accomplished based on decarboxylative iodination of acid 2 followed by "reattachment" of (14) C carboxylic function. The method allowed a significant reduction in the number of steps in preparation of the radiolabeled compound. Iodide 4, obtained by the halodecarboxylation, was converted to cyanide 5-[(14) C], which was hydrolyzed to provide the radiolabeled acid 2-[(14) C]. Coupling with β-alanine fragment and hydrolysis of ester 6-[(14) C] completed the synthesis of the target molecule 1-[(14) C]...
December 1, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Sally Wagner, Rodrigo Teodoro, Winnie Deuther-Conrad, Mathias Kranz, Matthias Scheunemann, Steffen Fischer, Barbara Wenzel, Ute Egerland, Norbert Hoefgen, Jörg Steinbach, Peter Brust
Cyclic nucleotide phosphodiesterase 10A (PDE10A) regulates the level of the second messengers cAMP and cGMP in particular in brain regions assumed to be associated with neurodegenerative and psychiatric diseases. A better understanding of the pathophysiological role of the expression of PDE10A could be obtained by quantitative imaging of the enzyme by positron emission tomography (PET). Thus, in this study we developed, radiolabeled, and evaluated a new PDE10A radioligand, 8-bromo-1-(6-[(18) F]fluoropyridin-3-yl)-3,4-dimethylimidazo[1,5-a]quinoxaline ([(18) F]AQ28A)...
November 29, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Paul Allen, Ryan A Bragg, Moya Caffrey, Cecilia Ericsson, Michael J Hickey, Lee P Kingston, Charles S Elmore
As part of a Medicinal Chemistry programme aimed at developing a highly potent and selective Cathepsin C inhibitor, tritium, carbon-14 and stable isotope labelled materials were required. The synthesis of tritium labelled methanesulfonate 5 was achieved via catalytic tritiolysis of a chloro precursor, albeit at a low radiochemical purity of 67%. Tritium labelled AZD5248 was prepared via a 3-stage synthesis, utilising amide directed hydrogen isotope exchange. Carbon-14 and stable isotope labelled AZD5248 were successfully prepared through modifications of the medicinal chemistry synthetic route, enabling the use of available labelled intermediates...
November 21, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Kai Cao, John A Brailsford, Ming Yao, Janet Caceres-Cortes, Robert Espina, Samuel J Bonacorsi
Two regioisomeric glucuronide metabolites of dapagliflozin (BMS-512148) were synthesized and used to elucidate the structures of dapagliflozin metabolites observed in human urine samples. The structures of the synthetic metabolites were assigned by HMBC, ROESY, and TOCSY experiments. Analogues of these metabolites containing carbon-13 as a stable-label were also prepared for use as internal standards for the analysis of urine samples obtained from patients participating in clinical studies. This article is protected by copyright...
November 21, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Ramesh Neelamegam, Daniel L Yokell, Peter A Rice, Shozo Furumoto, Yukitsuka Kudo, Nobuyuki Okamura, Georges El Fakhri
The radiotracer, [(18) F]-THK-5351 is a highly selective and high binding affinity PET imaging agent for aggregates of hyper-phosphorylated tau protein. Our report is a simplified one-pot, two-step radiosynthesis of [(18) F]-THK-5351. This report is broadly applicable for routine clinical production and multi-center trials on account of favorable half-life of flourine-18 and the use of a commercially available radiosynthesis module, the GE TRACERlab™ FXFN . First, the O-THP protected tosyl precursor underwent nucleophilic fluorinating reaction with potassium cryptand fluoride ([(18) F] fluoride (K[(18) F]/K222 )) in DMSO at 110 °C for 10 min followed by O-THP removal by using diluted hydrochloric acid (HCl) at same temperature...
November 17, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Jianguo Lin, Ling Qiu, Gaochao Lv, Ke Li, Wei Wang, Guiqing Liu, Xueyu Zhao, Shanshan Wang
Technetium-99 m-based radiopharmaceuticals have been used widely as diagnostic agents in the nuclear medicine. Chlorambucil (CLB) as one typical alkylating drug exhibits excellent inhibition effects against many human malignancies. In order to develop and explore a novel potential imaging agent for early diagnosis of tumors, tricarbonyl technetium-99 m and rhenium complexes based on the tridentate ligand dipicolylamine (DPA) bound to the chlorambucil pharmacophore were designed and synthesized: (99m) Tc-DPA-CLB (3) and Re-DPA-CLB (4)...
November 16, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Nafise Salek, Mohsen Mehrabi, Simindokht Shirvani Arani, Ali Bahrami Samani, Mostafa Erfani, Sara Vosoghi, Mohammad Ghannadi Maragheh, Mojtaba Shamsaei
In this study, the radiocomplexation of risedronic acid, a potent bisphosphonate with a no carrier added (NCA) (177) Lu, was investigated and followed by quality control studies, biodistribution evaluation, and dosimetry study for human based on biodistribution data in Wistar rats. The moderate energy β(-) emitter, (177) Lu (T½  = 6.7 days, Eβmax  = 497 keV), has been considered as a potential agent for development of bone-seeking radiopharmaceuticals. Because the specific activity of the radiolabeled carrier molecules should be high, the NCA radionuclides have an effective role in nuclear medicine...
November 15, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Melanie Cavani, Dirk Bier, Marcus Holschbach, Heinz H Coenen
An improved high yielding radiosynthesis of the known thiol-reactive maleimide-containing prosthetic group1-[3-(2-[(18) F]fluoropyridine-3-yloxy)propyl]pyrrole-2,5-dione ([(18) F]FPyME) is described. The target compound was obtained by a two-step one-pot procedure starting from a maleimide-containing nitro-precursor that was protected as a Diels-Alder adduct with 2,5-dimethylfurane. Nucleophilic radiofluorination followed by heat induced deprotection through a Retro Diels Alder reaction yielded, after chromatographic isolation, [(18) F]FPyME with a radiochemical yield of 20% in about 60 min overall synthesis time...
November 13, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Karoline T Neumann, Anders T Lindhardt, Benny Bang-Andersen, Troels Skrydstrup
A new synthetic route to the Tau binder, THK-523, is disclosed herein, which can easily be adapted to (13) C- and D-isotope labeling. The synthesis proceeds via two key reactions, namely, a Pd-catalyzed carbonylative Sonogashira coupling and a reductive ring-closing step with hydrogen or deuterium gas. By carrying out these reactions in a 2-chamber reactor we reported previously, ex situ-generated carbon monoxide and hydrogen/deuterium can be applied in stoichiometric quantities, thereby facilitating isotope labeling of this Tau-binding compound...
November 13, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Mythili Kameswaran, Vikram Gota, Rajwardhan Ambade, Sudeep Gupta, Ashutosh Dash
Trastuzumab that targets the human epidermal growth factor receptor type 2 (HER2) is known to benefit patients with HER2+ metastatic breast cancer. The objective was to explore the potential of (131) I-trastuzumab for treatment of breast cancers. Radioiodination of trastuzumab was carried out by chloramine-T method, purified by using PD-10 column, and characterized by size exclusion high-performance liquid chromatography on a gel column. In vitro studies were carried out in HER2+ cells to determine the specificity of the radioimmunoconjugate...
November 4, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
David Hesk, Carolee Lavey, Eric Soli
No abstract text is available yet for this article.
October 2, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Molahlehi S Sonopo, Adushan Pillay, Kelly Chibale, Biljana Marjanovic-Painter, Cristina Donini, Jan R Zeevaart
The antimalarial compound MMV390048 ([(14) C]-11) was labeled with carbon-14 isotope via a 3-step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon-14 labeled methyl iodide with a radiochemical purity of >99%. After single oral administration of [(14) C]-11 to albino and pigmented rats its tissue distribution profile was studied. Tissue distribution results showed high local exposure in the GI tract and excretory organs but low exposure of all other tissues. The radioactivity uptake was higher in the eyes of the pigmented rats than in the eyes of the albino rats at all-time points...
September 20, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Scott B Tran, Brad D Maxwell, Richard Burrell, Samuel J Bonacorsi
BMS-725519, BMS-811064, and BMS-812204 are potent and selective central cannabinoid receptor antagonists that have been investigated for the treatment of human obesity. To further understand their biotransformation profiles, radiolabelled and stable-labelled products were required. This paper describes the utility of [(14) C]1,1-carbonyldiimidazole as a radiolabelling reagent for the syntheses of carbonyl-labelled [(14) C]BMS-725519, [(14) C]BMS-811064, and [(14) C]BMS-812204. The syntheses of stable-labelled [(13) C6 ]BMS-725519 and [(13) CD3 (13) CD2 ]BMS-812204 synthesized from of [(13) C6 ]4-chloroacetophenone and [(13) CD3 (13) CD2 ]iodoethane, respectively, are also described...
September 14, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
David Hesk, Carolee Lavey, Eric Soli
No abstract text is available yet for this article.
September 13, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Mostafa Erfani, Zahra Shabani, Mojtaba Shamsaei, Seyed Pezhman Shirmardi, Mohammad Shafiei
In the present study paclitaxel (taxol) was labeled with [(99m) Tc(CO)3 (H2 O)3 ](+) core. Labeling was optimized, and radiochemical analysis was determined by thin layer chromatography and high performance liquid chromatography. Radiocomplex was evaluated and verified further as a tumor characterization agent in B16-F10 melanoma tumor-bearing mice. The [(99m) Tc(CO)3 (H2 O)3 ](+) -paclitaxel complex with high specific activity (0.77 GBq/μmol) and labeling yield (96.8 ± 1.3) was obtained. No decrease in labeling was observed up to 6 hours, and the stability of the radiocomplex was found adequate...
November 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Bachir Latli, Michael Stiasni, Matt Hrapchak, Zhibin Li, Nelu Grinberg, Heewon Lee, Carl A Busacca, Chris H Senanayake
Hyosine butyl bromide, the active ingredient in Buscopan, is an anticholinergic and antimuscarinic drug used to treat pain and discomfort caused by abdominal cramps. A straightforward synthesis of carbon-14- and deuterium-labeled Buscopan was developed using scopolamine, n-butyl-1-(14) C bromide, and n-butyl-(2) H9 bromide, respectively. In a second carbon-14 synthesis, the radioactive carbon was incorporated in the tropic acid moiety to follow its metabolism. Herein, we describe the detailed preparations of carbon-14- and deuterium-labeled Buscopan...
November 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Kai Sun, Chao Fang, Weicheng Yang, Zhongjie Xu, Haoran Wang, Wen Sun, Yong Luo, Yi Xu
This report presents an efficient synthesis of D6 -clenproperol and D6 -cimaterol with 99.5% and 99.7% isotopic abundance in acceptable yields and excellent chemical purities with deuterium isopropylamine as labelled precursor. Their structures and the isotope-abundance were confirmed by proton nuclear magnetic resonance and liquid chromatography-mass spectrometry.
November 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Zhongyi Yang, Huiyu Yuan, Xiaoping Xu, Bingxin Gu, Mingwei Wang, Jianping Zhang, Yongping Zhang, Yingjian Zhang
The purpose of the preliminary study was to investigate whether high specific activity (SA) of (18) F-fluoroestradiol was optimal in breast cancer diagnosis. Imaging at variable SA was conducted in a ZR-75-1 xenograft model of estrogen-receptor positive human breast cancer in 6 mice. The region of interest was manually drawn, and the percent of injected dose per gram of the tumor and muscle in the regions of interest were recorded. Tumor-to-muscle ratio (T/M) was calculated and compared in each group with different SAs...
November 2016: Journal of Labelled Compounds & Radiopharmaceuticals
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