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Journal of Labelled Compounds & Radiopharmaceuticals

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https://www.readbyqxmd.com/read/28670707/radiosynthesis-and-evaluation-of-1-substituted-3-2-3-dihydro-1h-inden-2-yl-6-1-ethylpropyl-3r-6r-2-5-piperazinedione-derivatives-as-pet-tracers-for-imaging-the-central-oxytocinergic-system
#1
Carmine Marzano, Steen Jacobsen, Cristian Salinas, Sac Pham Tang, Dirk Bender, Jan Passchier, Christophe Plisson
Oxytocin is known to be implicated in a variety of functions, such as learning, stress, anxiety, feeding and pain perception. Oxytocin is also important for social memory and attachment, human bonding, sexual and maternal behaviour, and aggression. Human disorders characterized by aberrant social interactions, such as autism and schizophrenia, may also involve abnormal oxytocin levels. GSK712043, GSK711320 and GSK664004, three antagonists exhibiting sub-nanomolar affinity for the human oxytocin receptor (hOTR) and high selectivity over vasopressin receptors were successfully labelled with carbon-11 with suitable yields (0...
July 3, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28640526/development-and-characterisation-of-a-99m-tc-tricarbonyl-labelled-estradiol-derivative-obtained-by-click-chemistry-with-potential-application-in-estrogen-receptors-imaging
#2
María Emilia Tejería, Javier Giglio, Silvia Dematteis, Ana Rey
Assessment of the presence of estrogen receptors in breast cancer is crucial for treatment planning. With the objective to develop a potential agent for estrogen receptors imaging we present the development and characterization of a (99m) Tc tricarbonyl labelled estradiol derivative. Using ethinylestradiol as starting material, a estradiol derivative bearing a 1,4-disubstituted 1,2,3-triazole-containing tridentate ligand system was synthesized by "Click Chemistry" and fully characterized. Labelling with high yield and radiochemical purity was achieved through the formation of a (99m) Tc-tricarbonyl complex...
June 22, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28631832/synthesis-of-two-carbon-14-analogue-of-thioflavanones
#3
Mohammad Basooti, Naghi Saadatjoo, Firozeh Nemati, Gholamhossein Shirvani, Mohammad Amin Ahmadi Faghih, Mohsen Javaheri
Thioflavanones are prevalent heterocyclic structural units in pharmaceutical and biologically active compound (Scheme1). In this paper, the synthesis of 2-phenylthiochroman-4-ones and 2-phenyl-4H-1-benzothiopyran-4-one labeled with carboxyl-14 is demonstrated.
June 20, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28626914/synthesis-preclinical-and-pharmacokinetic-evaluation-of-a-new-zoledronate-derivative-as-a-promising-antiosteoporotic-candidate-using-radiolabeling-technique
#4
H A Motaleb, I T Ibrahim, M El-Tawoosy, M I Mohamed
A novel zoledronic acid (ZL) derivative, 3-(2-ethyl-4-methyi-1H-imidazole-1-yl)-1-hydroxy-1-phosphonopropyl phosphonic acid (EMIHPBP), was synthesized, characterized and successfully radiolabeled with (99m) Tc. The in-vivo biodistribution of (99m) Tc-EMIHPBP was investigated and compared with the previously reported zoledronate derivatives aiming to formulate a novel zoledronate derivative with a high potential uptake to bone as a promising antiosteoporotic candidate. In order to further evaluate the bone uptake efficiency, the pharmacokinetics of (99m) Tc-EMIHPBP was investigated, and showed that maximum concentration in bone (Cmax ) was 31...
June 18, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28623878/in-vivo-characterisation-of-a-therapeutically-relevant-self-assembling-18-f-labelled-%C3%AE-sheet-forming-peptide-and-its-hydrogel-using-positron-emission-tomography
#5
O Morris, M A Elsawy, M Fairclough, K J Williams, A McMahon, J Grigg, D Forster, A F Miller, A Saiani, C Prenant
Positron emission tomography (PET) and fluorescence labelling have been used to assess the pharmacokinetics, biodistribution and eventual fate of a hydrogel-forming nonapeptide, FEFKFEFKK (F9) in healthy mice, using (18) F-labelled and fluoresceinisothiocyanate (FITC) - labelled F9 analogues. F9 was site-specifically radiolabelled with 2-[(18) F]fluoro-3-pyridinecarboxaldehyde ([(18) F]FPCA) via oxime bond formation. [(18) F]FPCA-F9 in vivo fate was evaluated both as a solution, following intravenous administration, and as a hydrogel when subcutaneously injected...
June 17, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28618064/technetium-99m-radiochemistry-for-pharmaceutical-applications
#6
REVIEW
Dionysia Papagiannopoulou
(99m) Tc is a widely used radionuclide and the development of (99m) Tc imaging agents continues to be in demand. This overview discusses basic principles of (99m) Tc radiopharmaceutical preparation and design, and focuses on the technetium-99m radiochemistry relevant to its medical applications. The (99m) Tc complexes are described based on the most typical examples in each category, keeping up with the state-of-the-art in the field. In addition, the main current strategies to develop targeted (99m) Tc radiopharmaceuticals are summarized...
June 15, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28600889/a-novel-versatile-precursor-suitable-for-18-f-radiolabelling-via-click-chemistry
#7
B Lugato, S Stucchi, S Ciceri, M N Iannone, E A Turolla, L Giuliano, C Chinello, S Todde, P Ferraboschi
As an effort to improve (18) F radiolabelling of biomolecules in terms of method robustness and versatility, we report the synthesis and radiolabelling of a new azido precursor potentially useful for the so called "click-reaction", in particular the ligand-free version of the copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC). The new azido precursor may help to overcome problems sometimes exhibited by most of the currently used analogues, as it is safe to handle and it displays long term chemical stability, thus facilitating the development of new radiolabelling procedures...
June 10, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28600824/preparation-of-68ga-mg-ca-phytate-colloid-and-its-evaluation-as-a-liver-imaging-agent
#8
Chris Tsopelas, William Hsieh
The objective of this study was to investigate the radiosynthesis of 68Ga-Mg-Ca-phytate colloid, and then characterise the formulation for radiochemical purity (RCP), radioactive particle size distribution, and biodistribution in normal rats. This radiocolloid was prepared by mixing an aqueous solution of phytic acid, 68Ga3+ ions, a dispersant, Mg2+ and Ca2+ ions, and then heating the contents at 100oC for 5 minutes. After cooling the vial to 5oC, the solution was basified to pH 5 and stored in the cold. The resulting product contained 92±3% RCP 68Ga-colloidal particles and a low level (8±3%) of soluble 68Ga-Mg-Ca-phytate...
June 10, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28600835/-in-loop-11-c-co2-fixation-prototype-and-proof-of-concept
#9
Kenneth Dahl, Thomas L Collier, Ran Chang, Xiaofei Zhang, Oleg Sadovski, Steven H Liang, Neil Vasdev
Carbon-11 labelled carbon dioxide is the most common feedstock for the synthesis of positron emission tomography radiotracers, and can be directly used for (11) C-carbonylation. Herein, we report the development of an apparatus that takes advantage of "in-loop" technologies to facilitate robust and reproducible syntheses of (11) C-carbonyl-based radiotracers by [(11) C]CO2 -fixation. Our "in-loop" [(11) C]CO2 -fixation method is simple, efficient, and proceeds smoothly at ambient pressure and temperature. We selected model (11) C-carbonyl labelled carbamates as well as symmetrical and unsymmetrical ureas based on their widespread use in radiotracer design and our clinical research interests for proof-of-concept...
June 9, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28561530/preparation-of-a-novel-radiotracer-targeting-the-ephb4-receptor-via-radiofluorination-using-spiro-azetidinium-salts-as-precursor
#10
Jens Wiemer, Jörg Steinbach, Jens Pietzsch, Constantin Mamat
The visualization of Eph receptors, which are overexpressed in various tumor entities, using selective small molecule Eph inhibitors by means of PET is a promising approach for tumor imaging. N-(Pyrimidinyl)indazolamines represent a class of compounds, which are known to have high affinity especially for the EphB4 receptor. Radiofluorination of these compounds could provide a highly specific imaging agent and was investigated using a classical nucleophilic introduction of [(18) F]fluoride as well as a less common nucleophilic ring opening reaction of azetidinium salts...
May 31, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28556976/exploring-the-radiosynthesis-and-in-vitro-characteristics-of-68-ga-ga-dota-siglec-9
#11
Svend B Jensen, Meeri Käkelä, Lars Jødal, Olli Moisio, Aage K O Alstrup, Sirpa Jalkanen, Anne Roivainen
Vascular adhesion protein 1 is a leukocyte homing-associated glycoprotein, which upon inflammation rapidly translocates from intracellular sources to the endothelial cell surface. It has been discovered that the cyclic peptide residues 283-297 of sialic acid-binding IgG-like lectin 9 (Siglec-9) "CARLSLSWRGLTLCPSK" bind to vascular adhesion protein 1 and hence makes the radioactive analogues of this compound ([(68) Ga]Ga-DOTA-Siglec-9) interesting as a noninvasive visualizing marker of inflammation. Three different approaches to the radiosynthesis of [(68) Ga]Ga-DOTA-Siglec-9 are presented and compared with previously published methods...
May 30, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28556950/the-radiosynthesis-of-novel-pi3k-inhibitor-8-ethoxy-2-4-18-f-fluorophenyl-3-nitro-2h-chromene-18-f-efpnc
#12
Jianfeng Liu, Jinrui Sun, Yuekai Li, Peng Su, Guihua Hou, Jiankui Han
8-ethoxy-2-(4-[(18) F]fluorophenyl)-3-nitro-2H-chromene((18) F-EFPNC)was preparated through nucleophilic substitution reaction of the precursor 8-ethoxy -2-[(4 -N, N, N-trimethylammonium triflate)phenyl]-3-nitro-2H-chromene and nuclide [(18) F] fluorination. The best radiosynthesis condition was obtained via [(18) F] fluorination substitution reaction between [(18) F] and 18 mg of the precursor in dimethyl sulfoxide(DMSO) at 150 °C for 5 min after the radiosynthesis method was optimized.The decay-corrected radiochemical yields(DCRY) of (18) F-EFPNC were 38...
May 30, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28545167/synthesis-of-s-2-s-3-4-chlorophenyl-n-4-chlorophenyl-sulfonyl-4-phenyl-4-5-dihydro-1h-pyrazole-1-carboximidamido-3-methyl-d3-butanamide-d5-octa-deuterated-jd5037
#13
Malliga R Iyer, Resat Cinar, Nathan J Coffey, Robert J Chorvat, George Kunos
JD5037 (1) is a potent and selective, peripherally acting inverse agonist of the cannabinoid (CB1 R) receptor. Peripheral CB1 receptor antagonists/inverse agonists have great potential in the treatment of metabolic disorders like type 2 diabetes, obesity and NASH. We report the synthesis of octa-deuterated [(2) H8 ]-JD5037 (S, S) (8) along with its (S, R) diastereomer (13) from commercially available L-valine-d8 starting material. The [(2) H8 ]-JD5037 compound will be used to quantitate unlabeled JD5037 during clinical ADME studies and will be used as an LC-MS/MS bioanalytical standard...
May 25, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28545160/-99m-tc-labeled-ngr-chlorambucil-conjugate-99m-tc-hynic-clb-c-ngr-for-targeted-chemotherapy-and-molecular-imaging
#14
Kusum Vats, Drishty Satpati, Rohit Sharma, Chandan Kumar, Haladhar D Sarma, Ashutosh Dash
Targeted delivery of chemotherapeutic drug at the tumor site enhances the efficacy with minimum systemic exposure. Towards this, drugs conjugated with peptides having affinity towards a particular molecular target are recognized as affective agents for targeted chemotherapy. Thus, in the present study, tumor-homing asparagine-glycine-arginine (NGR) peptide ligand was conjugated to DNA alkylating nitrogen mustard, chlorambucil (CLB). The peptide-drug conjugate (PDC), CLB-c(NGR), was radiolabeled with (99m) Tc-HYNIC core to trace its pharmacokinetics and biodistribution pattern...
May 25, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28543301/introducing-practitioner-protocols
#15
EDITORIAL
(no author information available yet)
No abstract text is available yet for this article.
May 19, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28512784/evaluation-of-aromatic-radiobromination-by-nucleophilic-substitution-using-diaryliodonium-salt-precursors
#16
Dong Zhou, Sung Hoon Kim, Wenhua Chu, Thomas Voller, John A Katzenellenbogen
Radiobromine-labeled compounds can be used for positron emission tomography (PET) imaging (ie, (76) Br) and for radiation therapy (ie, (77) Br). However, the commonly used electrophilic substitution reaction using no-carrier-added radiobromide does not always afford the desired product due to the high reactivity of the brominating intermediate. A nucleophilic substitution by bromide, such as radiobromination of iodonium precursors, provides an alternative route for the synthesis of bromo-radiopharmaceuticals...
May 17, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28494515/potent-and-selective-inhibitors-of-11%C3%AE-hydroxysteroid-dehydrogenase-type-1-labeled-with-carbon-13-and-carbon-14
#17
Bachir Latli, Matt Hrapchak, Jolaine Savoie, Yongda Zhan, Carl A Busacca, Chris H Senanayake
(S)-6-(2-Hydroxy-2-methylpropyl)-3-((S)-1-(4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl)ethyl)-6-phenyl-1,3-oxazinan-2-one (1) and (4aR,9aS)-1-(1H-benzo[d]midazole-5-carbonyl)-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-b]pyridine-6-carbonitrile hydrochloride (2) are potent and selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 enzyme. These 2 drug candidates developed for the treatment of type-2 diabetes were prepared labeled with carbon-13 and carbon-14 to enable drug metabolism, pharmacokinetics, bioanalytical, and other studies...
May 11, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28477391/a-mix-and-use-approach-for-formulation-of-human-clinical-doses-of-177-lu-dotmp-at-hospital-radiopharmacy-for-management-of-pain-arising-from-skeletal-metastases
#18
Sudipta Chakraborty, K V Vimalnath, A Rajeswari, Rubel Chakravarty, H D Sarma, E Radhakrishnan, K Kamaleshwaran, Ajit S Shinto, Ashutosh Dash
Use of bone-seeking radiopharmaceuticals is an established modality in the palliative care of pain due to skeletal metastases. (177) Lu-DOTMP is a promising radiopharmaceutical for this application owing to the ideally suited decay properties of (177) Lu and excellent thermodynamic stability and kinetic rigidity of the macrocyclic complex. The aim of the present study is to develop a robust and easily adaptable protocol for formulation of clinical doses of (177) Lu-DOTMP at hospital radiopharmacy. After extensive radiochemical studies, an optimized strategy for formulation of clinical doses of (177) Lu-DOTMP was developed, which involves simple mixing of approximately 3...
May 5, 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
#19
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 cholinesterase inhibitor that 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 imaging tracer for assessment of cholinesterases in live brain, peripheral tissues, and blood. However, the previously reported [(18) F]1 tracer synthesis was slow even with microwave acceleration, required high-performance liquid chromatography separation of the tracer from impurities, and gave less optimal radiochemical yields...
June 15, 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
#20
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...
May 30, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
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