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Journal of Labelled Compounds & Radiopharmaceuticals

Lee Kingston, Jonas Bergare, Hans Lönn, Cecilia Ericsson, Gunnar Grönberg, Song Chen, Charles S Elmore
In support of the development of a new treatment for COPD, two C-14 labeled compounds were required for in vitro animal studies. The synthesis of nitrile [(14) C]-1 was completed in 3 steps from C-14 labeled 4-bromobenzonitrile in accord with the previously developed medicinal chemistry route. The second compound, 2, did not possess an arylnitrile as did 1 which made the synthetic design more complex. An advanced, unlabeled benzotriazole containing intermediate, 10, was synthesized in low yield over 3 steps and was subsequently reacted with K(14) CN to give a mixture of diastereomers 12...
March 21, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Tiemen van Mourik, Michael Claesener, Klaas Nicolay, Holger Gruell
Fibrin deposition is observed in several diseases such as atherosclerosis, deep vein thrombosis and also tumors, where it contributes to the formation of mature tumor stroma. The aim of this study was to develop a gallium-labeled peptide tracer based on the fibrin targeting peptide Epep for PET imaging of fibrin deposition. For this purpose, the peptide Epep was modified with a NOTA moiety for radiolabeling with (67) Ga and (68) Ga and compared with the earlier validated (111) In-DOTA-Epep tracer. In vitro binding assays of (67) Ga-NOTA-Epep displayed an enhanced retention as compared to previously published data showing binding of (111) In-DOTA-Epep to human (84...
March 20, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Brad D Maxwell, Van Ly, Barry Brock, Robert Dodge, Mark Tirmenstein, Jacqueline Calvano
PEGylation is a proven approach to prolonging the duration of action and enhancing biophysical solubility and stability of peptides. 4-Acetylphenylalanine is a novel amino acid with a ketone side chain that is uniquely reactive in proteins. The ketone functionality can react with an amino-oxy functionalized PEG polymer to form a stable oxime adduct of the protein. One concern with using unnatural amino acids, such as 4-acetyl-phenylalanine, is the possibility of it being cleaved from the peptide and becoming incorporated into endogenous proteins...
March 8, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Brad D Maxwell
Type 2 diabetes is a significant worldwide health problem. To support the development of BMS-816336 as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) for type 2 diabetes, the synthesis of carbon-14 labeled material was required for use in metabolic profiling. [Phenyl-(14) C(U)]BMS-816336 was synthesized in 8 steps and 22% radiochemical yield from commercially available [(14) C(U)]bromobenzene. The radiochemical purity of [phenyl-(14) C(U)]BMS-816336 was 100% having a specific activity of 84...
March 8, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Christopher Dietz, Robert B Clark, Frank C Nichols, Michael B Smith
Bacterial serine dipeptide lipids are known to promote inflammatory processes and are detected in human tissues associated with periodontal disease or atherosclerosis. Accurate quantification of bacterial serine lipid, specifically lipid 654 [((S)-15-methyl-3-((13-methyltetradecanoyl)oxy)hexadecanoyl)glycyl-L-serine, (3S)-L-serine] isolated from Porphyromonas gingivalis,(1) in biological samples requires the preparation of a stable isotope internal standard for sample supplementation and subsequent mass spectrometric analysis...
March 8, 2017: 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
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...
March 2017: Journal of Labelled Compounds & Radiopharmaceuticals
Mingyue Kardashinsky, Nigel Lengkeek, Louis M Rendina
Delocalized lipophilic cations such as tri- and tetra-arylphosphonium are able to diffuse across the mitochondrial membrane, which allows them to selectively accumulate in cells with a high transmembrane potential (ΔΨm ). The mitochondrial membrane potential of cancer cells and cardiomyocytes has been reported to be significantly higher than that of normal epithelial cells. This feature can be exploited for the selective accumulation of phosphonium derivatives for the purposes of molecular imaging using radionuclides...
January 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
Tomáš Elbert, Mahadeo R Patil, Aleš Marek
A regiospecific and enantiospecific synthesis of tritium-labeled 28-homocastasterone is reported. Appropriate chlorocarbonate, efficiently synthesized from the starting 28-homocastasterone in an overall yield of 46%, undergoes catalytic tritium dechlorination by the T2 /Pd[0]/Et3 N system, providing 28-[3β-(3) H]homocastasterone, in a good yield, radiochemical purity (>97%), and with a high specific activity (5.8 Ci/mmol).
December 15, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
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