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Journal of Labelled Compounds & Radiopharmaceuticals

Jianping Liu, Huan Wang, Shuxia Wang, Qianqian Xue, Dawei Wang, Wang Hang, Huabei Zhang
Fatty acids are myocardial metabolic agent for detecting myocardial ischemia and infraction. However, no (99m) Tc-labeled fatty acids had potential use in clinical practice. In this study, (99m) Tc-CpTT-10-oxo-para-PPA (1d), (99m) Tc-CpTT-11-oxo-para-PPA (2d), (99m) Tc-CpTT-12-oxo-para-PPA (3d), (99m) Tc-CpTT-11-oxo-ortho-PPA (4d) and (99m) Tc-CpTT-11-oxo-meta-PPA (5d) were synthesized by a double ligand transfer reaction, their biological behaviors were investigated. Compound 2d achieved good heart/blood ratio (3...
February 9, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Thomas Lee Collier, Daniel L Yokell, Eli Livni, Peter A Rice, Sofie Celen, Kim Serdons, Ramesh Neelamegam, Guy Bormans, Dawn Harris, Abbas Walji, Eric D Hostetler, Idriss Bennacef, Neil Vasdev
Fluorine-18 labelled 6-(fluoro)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18) F]MK-6240) is a novel potent and selective PET radiopharmaceutical for detecting human neurofibrillary tangles, which are made up of aggregated tau protein. Herein, we report the fully automated two-step radiosynthesis of [(18) F]MK-6240 using a commercially available radiosynthesis module, GE Healthcare Tracerlab(TM) FXFN . Nucleophilic fluorination of the 5-diBoc-6-nitro precursor with potassium cryptand [(18) F]fluoride (K[(18) F]/K222 ) was carried out by conventional heating, followed by acid deprotection and semi-preparative HPLC under isocratic conditions...
February 9, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Martin A Hayes, Ieuan Roberts, Gunnar Grönberg, Kexin Lv, Baorui Lin, Jonas Bergare, Charles S Elmore
1β-hydroxydeoxycholic acid in unlabeled and stable isotope labeled forms was required for use as a biomarker for Cytochrome P450 3A4/5. A lengthy synthesis was undertaken to deliver the unlabeled compound and in the process, to develop a route to the deuterium labeled compound. The synthesis of the unlabeled compound was completed, but in very low yield. Concurrent with the synthetic approach, a biosynthetic route was pursued and this approach proved to be much more rapid and afforded the compound in both unlabeled and deuterium labeled forms in a one-step oxidation from deoxycholic acid and [D4 ]deoxycholic acid respectively...
February 9, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Mohini Guleria, Tapas Das, Chandan Kumar, Jeyachitra Amirdhanayagam, Haladhar D Sarma, Sharmila Banerjee
Rituximab is a monoclonal chimeric antibody which has been approved by US FDA for immunotherapy of Non-Hodgkins' lymphoma (NHL). Bexxar and Zevalin are the two other approved radiolabeled antibodies for radioimmunotherapy of NHL; however the fact that they are of murine origin reduces their treatment efficacy. To circumvent this, efforts have been made to radiolabel Rituximab with various therapeutic radioisotopes. In the present study, an effort has been made to optimize the conjugation (BFCA and antibody) and radiolabeling procedures for the preparation of clinical-scale (177) Lu-labeled Rituximab...
February 8, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Rashid Rasheed, Syed Ali Raza Naqvi, Syed Jawad Hussain Gillani, Ameer Fawad Zahoor, Asif Jielani, Nidda Saeed
The radiolabeled drug (99m) Tc-tazobactam ((99m) Tc-TZB) was developed and assessed as an infection imaging agent in P. aeruginosa and S. enterica infection induced animal models by comparing with inflammation induced animal models. Radiosynthesis of (99m) Tc-TZB was assessed while changing ligand concentration, reducing agent concentration, pH and reaction time while keeping radioactivity constant (~370 MBq). Percent labeling of the resulting complex was measured using paper chromatography and instant thin layer chromatography (ITLC-SG)...
February 8, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Kate Ellis-Sawyer, Ryan A Bragg, Nick Bushby, Charles S Elmore, Michael J Hickey
The aryl methyl group is found in many drug-like compounds, but there are limited ways of preparing compounds with an isotope label in this methyl position. The process of cyanation of an aryl halide followed by complete reduction of the nitrile to a methyl group was investigated as a route for preparing stable and radiolabelled isotopologues of drug-like compounds. Using this methodology, carbon-13, deuterium, carbon-14 and tritium labelled isotopologues of the non-steroidal anti-inflammatory drug (NSAID) tolmetin were produced, as well as carbon-13, deuterium and carbon-14 labelled isotopologues of another NSAID, celecoxib...
January 28, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Nematallah Mansour, Véronique Dumulon-Perreault, Samia Ait-Mohand, Michel Paquette, Roger Lecomte, Brigitte Guérin
In this study we investigated for the first time the influence of 2-aminoethyl-piperazine-1-carboxylic acid (APCA) and amino-hexanedioic-1-acid (AHDA) on tumor uptake and elimination kinetics of [(64) Cu]radiolabeled GRPR antagonists. Three GRPR antagonists containing the RM26 sequence were synthesized and conjugated with NOTA via different linkers (LK): polyethylene glycol (PEG-neutral), APCA (dicationic) or AHDA (dianionic). The NOTA-LK-RM26 peptides were radiolabeled with (64) Cu to assess their pharmacokinetic and positron emission tomography (PET) imaging properties using PC3 tumor-bearing athymic nude mice...
January 27, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
D Hesk, S Borges, R Dumpit, S Hendershot, D Koharski, P McNamara, S Ren, S Saluja, V Truong, K Voronin
MK 3814 is a potent and selective antagonist of the A2a receptor. A2a receptor antagonists have the potential for the treatment of Parkinson's disease. Three distinct isotopically labelled forms of MK 3814 were synthesized. [(3) H]MK 3814 was prepared for a preliminary ADME evaluation of the compound and [(14) C]MK 3814 for more definitive ADME work, including an AME study in man. In addition [(2) H4 ]MK 3814 was prepared as an internal standard for a LC-MS bioanalytical method. The paper discusses the synthesis of three isotopically labelled forms of MK 3814...
January 27, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Anna Krzyczmonik, Thomas Keller, Anna Kirjavainen, Sarita Forsback, Olof Solin
The chemistry of F2 and its derivatives are amenable to facile aliphatic or aromatic substitution, as well as electrophilic addition. The main limitation in the use of [(18) F]F2 for radiopharmaceutical synthesis is the low specific activity achieved by the traditional methods of production. The highest specific activities, 55 GBq/µmol, for [(18) F]F2 have been achieved so far by using electrical discharge in the post-target production of [(18) F]F2 gas from [(18) F]CH3 F. We demonstrate that [(18) F]F2 is produced by illuminating a gas mixture of neon/F2 /[(18) F]CH3 F with vacuum ultraviolet (VUV) photons generated by an excimer laser...
January 25, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Crist N Filer
This review discusses the synthetic methods used to tritiate nonmorphinan alkaloids as well as their applications.
January 10, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Naiara Vazquez, Stephan Missault, Christel Vangestel, Steven Deleye, David Thomae, Pieter Van der Veken, Koen Augustyns, Steven Staelens, Stefanie Dedeurwaerdere, Leonie Wyffels
MMP-9 is a zinc-dependent endopeptidase that is involved in the proteolytic degradation of the extracellular matrix and plays an important role in cancer migration, invasion, and metastasis. The aim of this study was to evaluate the potential of MMP-tracers [(18) F]BR420 and [(18) F]BR351 for MMP-9 imaging in a colorectal cancer xenograft model. [(18) F]BR420 and [(18) F]BR351 were synthesized using an automated synthesis module. For [(18) F]BR420, a novel and improved radiosynthesis was developed. Plasma stability and MMP-9-targeting capacity of both radiotracers was compared in the Colo205 colorectal cancer model...
December 21, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Lynda J Brown, Giuseppe Pileio, Malcolm H Levitt, Richard C D Brown
Unsymmetrical perdeuterated doubly (13) C labelled oxalates exhibit extended lifetimes in the nuclear singlet state. Synthesis of 1,2 (13) C2 oxalates from commercially available precursors is described, facilitating preparation of unsymmetrical oxalates in a controlled manner.
December 19, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Falguni Basuli, Xiang Zhang, Carolyn C Woodroofe, Elaine M Jagoda, Peter L Choyke, Rolf E Swenson
Fluorine-18 labeling of biomolecules is mostly performed by an indirect labeling method using a prosthetic group. Fluorine-18 labeled 6-fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester is a useful prosthetic group to radiolabel a protein. Recently, we reported an improved preparation of this prosthetic group. To test the conjugation efficiency of the labeled ester prepared by this method, we have performed conjugation reactions with a peptide, a protein, and a small molecule. Prostate-specific membrane antigen targeting small molecule [(18) F]DCFPyL, αvβ3 integrin receptors targeting peptide [(18) F]c(RGDfK) and [(18) F]albumin were prepared in good radiochemical yields...
December 18, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Tomáš Elbert, Mahadeo R Patil, Aleš Marek
No abstract text is available yet for this article.
December 15, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Pavel Barta, Jiri Janousek, Katerina Zilkova, Frantisek Trejtnar
Radioimmunoassay belongs to the analytical method enabling highly specific and sensitive quantification of molecules. The verification of the real-time radioimmunoassay technology usefulness for ligand-quality characteristics evaluation such as concentration, influence of radiolabeling on binding affinity and stability was estimated. The anti-epidermal growth factor receptor antibody (131) I-cetuximab was employed as the ligand antibody. The concentration of (131) I-cetuximab was derived from the shape of binding curves coming from the ligand-receptor interaction...
December 13, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Brad D Maxwell, Scott B Tran
Tetrazoles are a common heterocyclic functionality in many biologically active molecules. [1-(14) C]2-(1H-Tetrazol-5-yl)acetic acid was required as an intermediate in the synthesis of a development candidate as part of a discovery phase program to complete metabolic profiling studies. [1-(14) C]2-(1H-Tetrazol-5-yl)acetic acid was prepared in 4 steps overall and in 3 radiochemical steps from K(14) CN in an overall 32% radiochemical yield.
December 13, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Gholamhossein Shirvani, Abbas Shockravi, Mohsen Amini, Nader Saemian
Metallo-beta-lactamase enzymes make bacteria resistant to a broad range of commonly used beta-lactam antibiotics. Several thiol derivatives of L-amino acids have been shown their inhibitory effects against the metallo-β-lactamase IMP-1. In this study, (2-mercaptoacetyl)-L-tryptophan as a new inhibitor of metallo-β-lactamases labeled with carbon-14 in the 2-position of the indole ring was prepared from [2-(14) C]indole as a key synthetic intermediate based on chiral pool strategy. The overall synthesis was performed in 10 steps with the overall radiochemical yield 3...
December 12, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
Amsler Phillip, Wolf Thierry, Lanshoeft Christian, Bettighofer Anja, Eisfeld Jochen, Moenius Thomas, Probst Claudia, Etter Coralie, Heudi Olivier
Here, we describe the production of stable isotope-labeled human immunoglobulin G1 ([(13) C]-hIgG1) using [(13) C]-L-lysine/arginine-labeled hIgG1. The fermentation process was run in shake flasks containing labeled arginine and lysinethat were incorporated into the produced recombinant hIgG1. The [(13) C]-hIgG1 was purified, and label incorporation was determined to be >99% at all lysine and arginine moieties. Sequence coverage was confirmed by peptide mapping. [(13) C]-hIgG1 was then used as an internal standard (IS) for the development of a liquid chromatography-tandem mass spectrometry method applicable to the quantitative analysis of all human types of hIgG1 in rat serum...
December 12, 2016: 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
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