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Journal of Labelled Compounds & Radiopharmaceuticals

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https://www.readbyqxmd.com/read/28432800/effect-of-n-methyl-deuteration-on-pharmacokinetics-and-pharmacodynamics-of-enzalutamide
#1
Xuehai Pang, Lingling Peng, Yuanwei Chen
Enzalutamide, a 2nd generation antiandrogen, has been developed for the treatment of CRPC. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger anti-tumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin.
April 22, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28430366/cyclic-rgd-penta-peptides-crgdyk-derivatized-with-cyclopentadienyl-complexes-of-technetium-and-rhenium-as-radiopharmaceutical-probes
#2
Qaisar Nadeem, Yunjun Shen, Muhammad Farooq Warsi, Gulfam Nasar, Muhammad Abdul Qadir, Roger Alberto
The present study reports the syntheses of half-sandwich complexes of the type [M(η(5) -C5 H4 CONH-R)(CO)3 ] (M = Re,(99m) Tc;R = cyclic RGD peptide (cRGDyK) for potential imaging of αv β3 integrin expression. The (99m) Tc complex was prepared directly from the reaction of [(99m) Tc(OH2 )3 (CO)3 ](+) with cRGDyK, doubly conjugated to Thiele's acid [(C5 H5 COOH)2 ] in water. This approach extends the viability of metal-mediated retro Diels-Alder reactions for the preparation of small molecules such as linear tripeptides to a more complex cyclic peptide carrying a [(η(5) -C5 H4 )(99m) Tc(CO)3 ] tag...
April 21, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28423195/noninvasive-imaging-of-c-rgd-2-9r-as-a-potential-delivery-carrier-for-transfection-of-sirna-in-malignant-tumors
#3
Xue Qi Chen, Meng Liu, Rong Fu Wang, Ping Yan, Chun Li Zhang, Chao Ma, Qian Zhao, Lei Yin, Guang Yu Zhao, Feng Qin Guo
The purpose of our study was to develop and evaluate a novel integrin αv β3 -specific delivery carrier for transfection of siRNA in malignant tumors. We adopted arginine-glycine-aspartate (RGD) motif as a tissue target for specific recognition of integrin αν β3 . A chimaeric peptide was synthesized by adding nonamer arginine residues (9R) at the carboxy terminus of cyclic-RGD dimer, designated as c(RGD)2 -9R, to enable siRNA binding. To test the applicability of the delivery carrier in vivo, c(RGD)2 -9R was labeled with radionuclide of technetium-99 m...
April 18, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28419528/an-updated-synthesis-of-11-c-carfentanil-for-positron-emission-tomography-pet-imaging-of-the-%C3%AE-opioid-receptor
#4
Joseph E Blecha, Bradford D Henderson, Brian G Hockley, Henry F VanBrocklin, Jon-Kar Zubieta, Alexandre F DaSilva, Michael R Kilbourn, Robert A Koeppe, Peter J H Scott, Xia Shao
[(11) C]Carfentanil ([(11) C]CFN) is a selective radiotracer for in vivo positron emission tomography (PET) imaging studies of the μ-opioid system that, in our laboratories, is synthesized by methylation of the corresponding carboxylate precursor with [(11) C]MeOTf, and purified using a C2 solid-phase extraction cartridge. Changes in the commercial availability of common C2 cartridges have necessitated future-proofing the synthesis of [(11) C]CFN to maintain reliable delivery of the radiotracer for clinical imaging studies...
April 17, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28407286/pet-imaging-with-copper-64-as-a-tool-for-real-time-in-vivo-investigations-of-the-necessity-for-crosslinking-of-polymeric-micelles-in-nanomedicine
#5
Andreas I Jensen, Tina Binderup, Pramod Kumar Ek, Constance E Grandjean, Palle H Rasmussen, Andreas Kjaer, Thomas L Andresen
Polymeric micelles in nanomedicine are often crosslinked to prevent disintegration in vivo. This typically requires clinically problematic chemicals or laborious procedures. In addition, crosslinking may interfere with advanced release strategies. Despite this, it is often not investigated whether crosslinking is necessary for efficient drug delivery. We used PET imaging with (64) Cu to demonstrate general methodology for real-time in vivo investigations of micelle stability. Triblock copolymers with 4-methylcoumarin cores of ABC-type (PEG-PHEMA-PCMA) were functionalized in the handle region (PHEMA) with CB-TE2A chelators...
April 13, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28406535/burgess-iridium-i-catalyst-for-selective-hydrogen-isotope-exchange
#6
Annina Burhop, Raphail Prohaska, Remo Weck, Jens Atzrodt, Volker Derdau
We have evaluated the commercially available Burgess catalyst in Hydrogen Isotope Exchange (HIE) reactions with several substrates bearing different directing group functionalities and have obtained moderate to high (50-97%D) deuterium incorporations. The broad applicability in HIE reactions makes the Burgess catalyst a possible alternative compared to other commercially available iridium(I)catalysts.
April 12, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28406525/an-improved-radiosynthesis-of-o-2-18-f-fluoroethyl-o-p-nitrophenyl-methylphosphonate-a-first-in-class-cholinesterase-pet-tracer
#7
Kiel D Neumann, Charles M Thompson, Joseph E Blecha, John M Gerdes, Henry F VanBrocklin
O-(2-Fluoroethyl)-O-(p-nitrophenyl) methylphosphonate 1 is an organophosphate (OP) cholinesterase inhibitor, which creates a phosphonyl-serine covalent adduct at the enzyme active site blocking cholinesterase activity in vivo. The corresponding radiolabeled O-(2-[(18) F]fluoroethyl)-O-(p-nitrophenyl) methylphosphonate, [(18) F]1, has been previously prepared and found to be an excellent positron emission tomography (PET) imaging tracer for assessment of cholinesterases in live brain, peripheral tissues and blood...
April 12, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28370543/automated-synthesis-of-n-2-18-f-fluoropropionyl-l-glutamic-acid-as-an-amino-acid-tracer-for-tumor-imaging-on-a-modified-18-f-fdg-synthesis-module
#8
Shaoyu Liu, Aixia Sun, Zhanwen Zhang, Xiaolan Tang, Dahong Nie, Hui Ma, Shende Jiang, Ganghua Tang
N-(2-[(18) F]Fluoropropionyl)-L-glutamic acid ([(18) F]FPGLU) is a potential amino acid tracer for tumor imaging with positron emission tomography (PET). However, due to the complicated multi-step synthesis, the routine production of [(18) F]FPGLU presents many challenging laboratory requirements. In order to simplify the synthesis process of this interesting radiopharmaceutical, an efficient automated synthesis of [(18) F]FPGLU was performed on a modified commercial FDG synthesizer via a two-step on-column hydrolysis procedure, including (18) F-fluorination and on-column hydrolysis reaction...
April 3, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28370273/synthesis-of-specific-deuterated-derivatives-of-the-long-chained-stratum-corneum-lipids-eos-and-eop-and-characterization-using-neutron-scattering
#9
Stefan Sonnenberger, Adina Eichner, Thomas Schmitt, Thomas Hauß, Stefan Lange, Andreas Langner, Reinhard H H Neubert, Bodo Dobner
The synthesis of specific deuterated derivatives of the long chained ceramides [EOS] and [EOP] is described. The structural differences with respect to the natural compounds are founded in the substitution of the two double bond containing linoleic acid by a palmitic acid branched with a methyl group in 10-position. The specific deuteration is introduced both in the branched and in the terminal methyl group which was realized by common methods of successive deuteration of carboxylic groups in three steps. These modified fatty acids resp...
April 1, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28349626/study-of-n-vinylpyrrolidone-n-vinylformamide-copolymers-labelled-with-indium-113%C3%A2-m
#10
N I Gorshkov, A E Miroslavov, I E Alekseev, A A Lumpov, A Yu Murko, I I Gavrilova, N N Saprykina, M A Bezrukova, A I Kipper, V D Krasikov, D N Suglobov, M Yu Tyupina, E F Panarin
The procedure of the directed synthesis of N-vinylpyrrolidone-N-vinylformamide (VP-VFA) copolymers with grafted iminodiacetate (IDA) chelating units is presented. The methods for labelling resulting conjugates with indium-113 m were developed. The metal-copolymer conjugates were characterized by different physicochemical methods, including IR and NMR, viscometry, light scattering, and exclusion HPLC. Parameters of radiochemical synthesis of the conjugates labelled with indium-113 m were optimized. It was shown that the VP-VFA-IDA copolymer firmly binds indium-113 m both in the acid and alkaline solutions, with pH of the reaction mixture having almost no effect on the complexation...
March 27, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28324911/synthesis-of-two-c-14-labeled-cathepsin-c-inhibitors-the-use-of-a-cyanide-to-displace-a-benzotriazole
#11
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
https://www.readbyqxmd.com/read/28317154/development-of-a-novel-fibrin-specific-pet-tracer
#12
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
https://www.readbyqxmd.com/read/28273378/the-synthesis-of-14-c-4-acetylphenylalanine-effect-on-cell-viability-and-assessment-of-protein-incorporation-in-male-rat-hepatocytes
#13
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
https://www.readbyqxmd.com/read/28273377/the-syntheses-of-13-c6-and-phenyl-14-c-u-bms-816336-an-inhibitor-of-11%C3%AE-hydroxysteroid-dehydrogenase-type-1-for-type-2-diabetes
#14
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
https://www.readbyqxmd.com/read/28271544/convergent-synthesis-of-a-deuterium-labeled-serine-dipeptide-lipid-for-analysis-of-biological-samples
#15
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, 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
https://www.readbyqxmd.com/read/28185309/initial-evaluation-of-99m-tc-tricarbonyl-cyclopentadienyl-fatty-acids-derivatives-as-spect-tracers-for-myocardium
#16
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
https://www.readbyqxmd.com/read/28185305/cgmp-production-of-the-radiopharmaceutical-18-f-mk-6240-for-pet-imaging-of-human-neurofibrillary-tangles
#17
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
https://www.readbyqxmd.com/read/28183147/synthesis-of-1%C3%AE-hydroxydeoxycholic-acid-in-h-2-and-unlabeled-forms
#18
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 activity. 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 a 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 1-step oxidation from deoxycholic acid and [D4 ]deoxycholic acid, respectively...
February 9, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28181275/preparation-of-clinical-scale-177-lu-rituximab-optimization-of-protocols-for-conjugation-radiolabeling-and-freeze-dried-kit-formulation
#19
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
https://www.readbyqxmd.com/read/28181269/-99m-tc-tazobactam-a-novel-infection-imaging-agent-radiosynthesis-quality-control-biodistribution-and-infection-imaging-studies
#20
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
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