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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...
October 26, 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...
October 17, 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.
October 17, 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...
October 13, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Yahui Tu, Jiaqi Zhong, Haoran Wang, Jie Pan, Zhongjie Xu, Weicheng Yang, Yong Luo
Three stable and simple synthetic routes of labeled D9 -Mabuterol, D9 -Bambuterol, and D9 -Cimbuterol were described with 98.5%, 99.7%, and 98.4% isotopic abundance and good purity. These structures and isotope-abundance were confirmed according to (1) H NMR and liquid chromatography-tandem mass spectrometry.
October 13, 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
Hiroyuki Kimura, Yusuke Yagi, Kenji Arimitsu, Kazuya Maeda, Kazuaki Ikejiri, Jun-Ichi Takano, Hiroyuki Kusuhara, Shinya Kagawa, Masahiro Ono, Yuichi Sugiyama, Hideo Saji
Pitavastatin is an antihyperlipidemic agent, a potent inhibitor of 3-hydroxymethyl-glutaryl-CoA reductase, which is selectively taken up into the liver mainly via hepatic organic anion transporting polypeptide 1B1 (OATP1B1). OATP1B1 can accept a variety of organic anions, and previous reports indicated that it is responsible for the hepatic clearance of several clinically used anionic drugs. Therefore, the pharmacokinetics and the hepatic distribution of pitavastatin provide an insight into the function of OATP1B1 in humans...
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
Douglas E Stack, Rachel Eastman
Regioselective labelling of arene rings via electrophilic exchange is often dictated by the electronic environment caused by substituents present on the aromatic system. Previously, we observed the presence of a t-butyl group, either covalently bond or added as an external reagent, could impart deuterium exchange to the unactivated, C1-position of estrone. Here, we provide nuclear magnetic resonance analysis of this exchange in a solvent system composed of 50:50 trifluoroacetic acid and D2 O with either 2-t-butylestrone or estrone in the presence of t-butyl alcohol has shed insights into the mechanism of this t-butyl-catalyzed exchange...
October 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Stefan Sonnenberger, Stefan Lange, Andreas Langner, Reinhard H H Neubert, Bodo Dobner
The synthesis of 12 deuterated ceramides with either a deuteration at the last carbon atom of the amide bound fatty acid or a perdeuterated fatty acid chain is described. The ceramides were prepared starting from sphingosine or phytosphingosine and ω deuterated or perdeuterated fatty acids with PyBOP® as activating agent in high yields. For the synthesis of the specifically deuterated fatty acids, dicarboxylic acids were transformed into ω deuterated alkyl bromide, which was chain elongated with blocked ω bromo alcohols by copper catalyzed Grignard coupling...
October 2016: Journal of Labelled Compounds & Radiopharmaceuticals
M H Sanad, Kh M Sallam, F A Marzook, S M Abd-Elhaliem
The goal of the study aims to evaluate newly radioiodinated candesartan (CAN) as a potential cardiovascular tracer. CAN was labeled using (125) I with chloramine-T (Ch-T) and N-bromosuccinimide (NBS) with full characterization of cold Iodo-candesartan. Factors such as pH, reaction temperature, reaction time, substrate, and oxidizing agent amounts were studied to optimize the radioiodination of CAN. The optimum radiochemical yield of (125) I-CAN was 98%. The labeled compound was separated and purified using high-pressure liquid chromatography...
October 2016: Journal of Labelled Compounds & Radiopharmaceuticals
A Virgone-Carlotta, E Dufour, S Bacot, M Ahmadi, M Cornou, L Moni, J Garcia, S Chierici, D Garin, D Marti-Batlle, P Perret, J F Ghersi-Egea, M Moulin Sallanon, D Fagret, C Ghezzi
New strategies allowing the transfer of molecules, especially peptides, through the blood-brain barriers are a major pharmacological challenge for the treatment of brain diseases. The present study aims at evaluating in vivo the cerebral bioavailability of carrier systems, based on small and functionalizable 2,5-diketopiperazine (DKP) motifs. We studied 2 different cyclo(Lys-Lys) DKP scaffolds alone and a cyclo(Lys-Gly) DKP carrier bearing as peptide model, the tau protein hexapeptide VQIVYK sequence. The different carrier systems were synthesized and radiolabeled using one of the free domains...
October 2016: Journal of Labelled Compounds & Radiopharmaceuticals
William Hsieh, Masood Ali, Renee Praehofer, Chris Tsopelas
The objective of this study was to investigate the radiosynthesis of (68) Ga-Ca-phytate particles and then characterize the formulation for radiochemical purity, radioactive particle size distribution, and biodistribution in normal rats. This radiotracer was prepared using a commercial phytate cold kit after reconstitution with saline, (68) Ga-chloride generator eluent, calcium chloride, and air, then heating at 100°C for 30 minutes to achieve 99% radiochemical purity of (68) Ga-particles that were 21% 3-5 μm, 8% 5-15 μm, and 71% >15 μm in diameter...
October 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Phoebe Y H Lam, Christopher R T Hillyar, Sarah Able, Katherine A Vallis
The surface overexpression of nucleolin provides an anchor for the specific attachment of biomolecules to cancer and angiogenic endothelial cells. The peptide F3 is a high-affinity ligand of the nucleolin receptor (NR) that has been investigated as a carrier to deliver biologically active molecules to tumors for both therapeutic and imaging applications. A site-specific PEGylated F3 derivative was radiolabeled with [(18) F]Al-F. The binding affinity and cellular distribution of the compound was assessed in tumor (H2N) and tumor endothelial (2H-11) cells...
October 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Aleš Marek, Martin H F Pedersen, Stine B Vogensen, Rasmus P Clausen, Bente Frølund, Tomáš Elbert
3-Hydroxycyclopent-1-ene-1-carboxylic acid (HOCPCA (1)) is a potent ligand for high-affinity γ-hydroxybutyric acid binding sites in the central nervous system. Various approaches to the introduction of a hydrogen label onto the HOCPCA skeleton are reported. The outcomes of the feasible C─H activation of olefin carbon (C-2) by iridium catalyst are compared with the reduction of the carbonyl group (C-3) by freshly prepared borodeuterides. The most efficient iridium catalysts proved to be Kerr bulky phosphine N-heterocyclic species providing outstanding deuterium enrichment (up to 91%) in a short period of time...
October 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Zhengxing Zhang, Chengcheng Zhang, Joseph Lau, Nadine Colpo, François Bénard, Kuo-Shyan Lin
4-[(18) F]Fluorobenzyltriphenylphosphonium cation ((18) F-FBnTP) is a promising negative membrane potential targeting positron emission tomography tracer. However, the reported multistep radiolabeling approach for the synthesis of (18) F-FBnTP poses a challenge for routine clinical applications. In this study, we demonstrated that (18) F-FBnTP can be prepared in good conversion yields (~60%, nondecay corrected) in just one step via a copper-mediated (18) F-fluorination reaction using a pinacolyl arylboronate precursor...
September 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Stephanie Doll, Karen Woolum, Krishan Kumar
A simple and rapid nonradioactive iodide labeling/radiolabeling method for peptides, using an inexpensive oxidizing agent such as sodium hypochlorite and a cyclic peptide, cRGDyK (cyclo Arg-Gly-Asp-d-Tyr-Lys), was developed in this work. Labeling reaction was optimized by conducting experiments under variable ratios of the reagents, the reaction times, and the pH. The study demonstrated that radiolabeling of the cyclic peptide was fast and pH independent. Monoiodinated and di-iodinated cRGDyK were formed under all conditions and varied with the ratio of the reagents and the reaction time...
September 2016: Journal of Labelled Compounds & Radiopharmaceuticals
M A Motaleb, M Abo-Kul, Samy M Ibrahim, Shokry M Saad, Muhammad Arafat
The preparation of (125) I-lamivudine ((125) I-3TC) and (125) I-lamivudine-ursodeoxycholic acid codrug ((125) I-3TC-UDCA), suitable for comparative biodistribution studies, is described. The synthesis of the unlabeled precursor 3TC-UDCA proceeds in an 11.6% yield, and the radiolabelling yields for (125) I-3TC and (125) I-3TC-UDCA were 89 and 92%, respectively. The final products are radiochemically pure (greater than 98%).
September 2016: Journal of Labelled Compounds & Radiopharmaceuticals
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