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Nuclear Medicine and Biology

Anneli Rydén, Görel Nyman, Lovisa Nalin, Susanne Andreasson, Olle Korsgren, Olof Eriksson, Marianne Jensen-Waern
No abstract text is available yet for this article.
September 7, 2016: Nuclear Medicine and Biology
William C Eckelman
No abstract text is available yet for this article.
September 3, 2016: Nuclear Medicine and Biology
Mika Naganawa, Shu-Fei Lin, Keunpoong Lim, David Labaree, Jim Ropchan, Paul Harris, Yiyun Huang, Masanori Ichise, Richard E Carson, Gary W Cline
INTRODUCTION: (18)F-Fluoropropyl-(+)-dihydrotetrabenazine ((18)F-FP-(+)-DTBZ) is a vesicular monoamine transporter type 2 (VMAT2) radiotracer for positron emission tomography (PET) imaging to quantify human β-cell mass. Renal cortex and spleen have been suggested as reference regions, however, little is known about (18)F-FP-(+)-DTBZ binding in these regions including the fraction of radiometabolite. We compared the kinetics of (18)F-FP-(+)-DTBZ and its inactive enantiomer (18)F-FP-(-)-DTBZ in baboons, estimated the non-displaceable binding (VND) of the tracers, and used ex vivo studies to measure radiometabolite fractions...
September 2, 2016: Nuclear Medicine and Biology
Dustin Wayne Demoin, Ashley N Dame, William D Minard, Fabio Gallazzi, Gary L Seickman, Tammy L Rold, Nicole Bernskoetter, Michael E Fassbender, Timothy J Hoffman, Carol A Deakyne, Silvia S Jurisson
INTRODUCTION: Targeted radiotherapy using the bifunctional chelate approach with (186/188)Re(V) is challenging because of the susceptibility of monooxorhenium(V)-based complexes to oxidize in vivo at high dilution. A monoamine-monoamide dithiol (MAMA)-based bifunctional chelating agent was evaluated with both rhenium and technetium to determine its utility for in vivo applications. METHODS: A 222-MAMA chelator, 222-MAMA(N-6-Ahx-OEt) bifunctional chelator, and 222-MAMA(N-6-Ahx-BBN(7-14)NH2) were synthesized, complexed with rhenium, radiolabeled with (99m)Tc and (186)Re (carrier added and no carrier added), and evaluated in initial biological distribution studies...
August 31, 2016: Nuclear Medicine and Biology
Davide Carta, Nicola Salvarese, Nicolò Morellato, Feng Gao, Wiebke Sihver, Hans Jurgen Pietzsch, Barbara Biondi, Paolo Ruzza, Fiorenzo Refosco, Debora Carpanese, Antonio Rosato, Cristina Bolzati
The purpose of this study was to evaluate the effect of cyclization on the biological profile of a [(99m)Tc(N)(PNP3)]-labeled α-melanocyte stimulating hormone peptide analog. A lactam bridge-cyclized H-Cys-Ahx-βAla(3)-c[Lys(4)-Glu-His-D-Phe-Arg-Trp-Glu(10)]-Arg(11)-Pro-Val-NH2 (NAP-NS2) and the corresponding linear H-Cys-Ahx-βAla-Nle-Asp-His-D-Phe-Arg-Trp-Gly-NH2 (NAP-NS1) peptide were synthetized, characterized by ESI-MS spectroscopy and their melanocortin-1 receptor (MC1R) binding affinity was determined in B16/F10 melanoma cells...
August 31, 2016: Nuclear Medicine and Biology
Falguni Basuli, Xiang Zhang, Elaine M Jagoda, Peter L Choyke, Rolf E Swenson
Fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester has been successfully synthesized in an unprecedented way by flowing an acetonitrile solution of its quaternary ammonium salt precursor (N,N,N-trimethyl-5-((2,3,5,6-tetrafluorophenoxy)carbonyl)pyridin-2-aminium trifluoromethanesulfonate, 1) through an anion exchange cartridge. The fluorination reaction proceeded at room temperature without azeotropic drying of the fluoride. Over 75% conversion was observed with 10mg of precursor in 2:8, acetonitrile: t-butanol in 1min...
August 30, 2016: Nuclear Medicine and Biology
Sang-Gyu Lee, Kishore Gangangari, Teja Muralidhar Kalidindi, Blesida Punzalan, Steven M Larson, Naga Vara Kishore Pillarsetty
INTRODUCTION: Bone marrow is the soft tissue compartment inside the bones made up of hematopoietic cells, adipocytes, stromal cells, phagocytic cells, stem cells, and sinusoids. While [(18)F]-FLT has been utilized to image proliferative marrow, to date, there are no reports of particle based positron emission tomography (PET) imaging agents for imaging bone marrow. We have developed copper-64 labeled liposomal formulation that selectively targets bone marrow and therefore serves as an efficient PET probe for imaging bone marrow...
August 27, 2016: Nuclear Medicine and Biology
Nathalie Rizzo-Padoin, Michael Chaussard, Nicolas Vignal, Ewa Kotula, Vadim Tsoupko-Sitnikov, Sofia Vaz, Fortune Hontonnou, Wang-Qing Liu, Jean-Luc Poyet, Michel Vidal, Pascal Merlet, Benoit Hosten, Laure Sarda-Mantel
INTRODUCTION: Melanoma is a highly malignant cutaneous tumor of melanin-producing cells. MEL050 is a synthetic benzamide-derived molecule that specifically binds to melanin with high affinity. Our aim was to implement a fully automated radiosynthesis of [(18)F]MEL050, using for the first time, the AllInOne™ synthesis module (Trasis), and to evaluate the potential of [(18)F]MEL050 for the detection of pigmented melanoma in mice primary subcutaneous tumors and pulmonary metastases, and to compare it with that of [(18)F]FDG...
August 24, 2016: Nuclear Medicine and Biology
Hojjat Ahmadzadehfar, Markus Essler, Michael Schäfers, Kambiz Rahbar
No abstract text is available yet for this article.
August 13, 2016: Nuclear Medicine and Biology
Tapas Das, Mohini Guleria, Sharmila Banerjee
No abstract text is available yet for this article.
August 13, 2016: Nuclear Medicine and Biology
Redmond-Craig Anderson, Mehran Makvandi, Kuiying Xu, Brian P Lieberman, Chenbo Zeng, Daniel A Pryma, Robert H Mach
BACKGROUND: PARP inhibitors (PARPi) have the potential to impact cancer therapy in a selective patient population; however, despite current patient selection methods clinical trials have shown mixed response rates. It is therefore clinically useful to determine which patients will respond prior to receiving PARPi therapy. One essential biomarker is to measure the level of PARP enzyme expression in tumors. Small molecule radiotracers have been developed to accurately quantify PARP-1 expression in vitro and in vivo...
August 12, 2016: Nuclear Medicine and Biology
Maroor Raghavan Ambikalmajan Pillai, Raviteja Nanabala, Ajith Joy, Arun Sasikumar, Furn F Russ Knapp
Because of the broad incidence, morbidity and mortality associated with prostate-derived cancer, the development of more effective new technologies continues to be an important goal for the accurate detection and treatment of localized prostate cancer, lymphatic involvement and metastases. Prostate-specific membrane antigen (PSMA; Glycoprotein II) is expressed in high levels on prostate-derived cells and is an important target for visualization and treatment of prostate cancer. Radiolabeled peptide targeting technologies have rapidly evolved over the last decade and have focused on the successful development of radiolabeled small molecules that act as inhibitors to the binding of the N-acetyl-l-aspartyl-l-glutamate (NAAG) substrate to the PSMA molecule...
August 11, 2016: Nuclear Medicine and Biology
Masayuki Hanyu, Kazunori Kawamura, Makoto Takei, Kenji Furutsuka, Satoshi Shiomi, Tomoya Fujishiro, Masanao Ogawa, Nobuki Nengaki, Hiroki Hashimoto, Toshimitsu Fukumura, Ming-Rong Zhang
INTRODUCTION: Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]-1-(6-[(11)C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([(11)C]TASP457, [(11)C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [(11)C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [(11)C]2 for qualifying H3 receptors in human brain. In this paper, we report an efficient radiosynthesis of [(11)C]2 to obtain sufficient radioactivity and high quality for clinical application...
August 10, 2016: Nuclear Medicine and Biology
Anna Schweifer, Florian Maier, Walter Ehrlichmann, Denis Lamparter, Manfred Kneilling, Bernd J Pichler, Friedrich Hammerschmidt, Gerald Reischl
INTRODUCTION: Radiolabeled 2-nitroimidazoles (azomycins) are a prominent class of biomarkers for PET imaging of hypoxia. [(18)F]Fluoro-azomycin-α-arabinoside ([(18)F]FAZA) - already in clinical use - may be seen as α-configuration nucleoside, but enters cells only via diffusion and is not transported by cellular nucleoside transporters. To enhance image contrast in comparison to [(18)F]FAZA our objective was to (18)F-radiolabel an azomycin-2´-deoxyriboside with β-configuration ([(18)F]FAZDR, [(18)F]-β-8) to mimic nucleosides more closely and comparatively evaluate it versus [(18)F]FAZA...
August 9, 2016: Nuclear Medicine and Biology
Iljung Lee, Brian P Lieberman, Shihong Li, Catherine Hou, Mehran Makvandi, Robert H Mach
INTRODUCTION: Nine novel analogues were synthesized including a 6-carbon spacer analogue of ISO-1 (7). They have moderate binding affinity for sigma-2 (σ2) receptors and high selectivity for σ2 receptors relative to sigma-1 (σ1) receptors. METHODS: ([(18)F]7) was synthesized and evaluated as a candidate ligand for positron emission (PET) imaging of the σ2 receptor in tumors. Radioligand [(18)F]7 was radiolabeled with (18)F via displacement of the corresponding mesylate precursor with [(18)F]fluoride...
August 9, 2016: Nuclear Medicine and Biology
Marian Meckel, Vojtěch Kubíček, Petr Hermann, Matthias Miederer, Frank Rösch
Radiolabeled bisphosphonates are commonly used in the diagnosis and therapy of bone metastases. Blood clearance of bisphosphonates is usually fast and only 30%-50% of the injected activity is retained in the skeleton, while most of the activity is excreted by the urinary tract. A longer blood circulation may enhance accumulation of bisphosphonate compounds in bone metastases. Therefore, a chemically modified macrocyclic bisphosphonate derivative with an additional human albumin binding entity was synthesized and pharmacokinetics of its complex was evaluated...
August 1, 2016: Nuclear Medicine and Biology
David S Geller, Jonathan Morris, Ekaterina Revskaya, Mani Kahn, Wendong Zhang, Sajida Piperdi, Amy Park, Pratistha Koirala, Hillary Guzik, Charles Hall, Bang Hoang, Rui Yang, Michael Roth, Jonathan Gill, Richard Gorlick, Ekaterina Dadachova
INTRODUCTION: Osteosarcoma overall survival has plateaued around 70%, without meaningful improvements in over 30years. Outcomes for patients with overt metastatic disease at presentation or who relapse are dismal. In this study we investigated a novel osteosarcoma therapy utilizing radioimmunotherapy (RIT) targeted to IGF2R, which is widely expressed in OS. METHODS: Binding efficiency of the Rhenium-188((188)Re)-labeled IGF2R-specific monoclonal antibody (mAb) to IGF2R on OS17 OS cells was assessed with Scatchard plot analysis...
July 30, 2016: Nuclear Medicine and Biology
Tomoyuki Ohya, Kotaro Nagatsu, Hisashi Suzuki, Masami Fukada, Katsuyuki Minegishi, Masayuki Hanyu, Toshimitsu Fukumura, Ming-Rong Zhang
INTRODUCTION: Copper-64 is an attractive radionuclide for positron emission tomography and is emerging as a radiotherapeutic agent. The demand of (64)Cu with low metallic impurities has increased because of its wide applications when incorporated with antibodies, peptides, and proteins. In this study, we propose a new separation method to produce high-quality (64)Cu using a cation exchange column, as well as an automated separation system suitable for large-scale production. METHODS: (64)Cu was produced from an electrodeposited (64)Ni target via the (64)Ni(p,n)-reaction with a 24MeV HH+ beam at 10eμA (electrical microampere) conducted for 1-3h...
July 30, 2016: Nuclear Medicine and Biology
Sara Neyt, Maarten Vliegen, Bjorn Verreet, Stef De Lombaerde, Kim Braeckman, Christian Vanhove, Maarten Thomas Huisman, Caroline Dumolyn, Ken Kersemans, Fabian Hulpia, Serge Van Calenbergh, Geert Mannens, Filip De Vos
INTRODUCTION: Hepatobiliary transport mechanisms are crucial for the excretion of substrate toxic compounds. Drugs can inhibit these transporters, which can lead to drug-drug interactions causing toxicity. Therefore, it is important to assess this early during the development of new drug candidates. The aim of the current study is the (radio)synthesis, in vitro and in vivo evaluation of a technetium labeled chenodeoxycholic and cholic acid analogue: [(99m)Tc]-DTPA-CDCA and [(99m)]Tc-DTPA-CA, respectively, as biomarker for disturbed transporter functionality...
October 2016: Nuclear Medicine and Biology
Dane Bergstrom, Jeffrey V Leyton, Arman Zereshkian, Conrad Chan, Zhongli Cai, Raymond M Reilly
INTRODUCTION: (111)In-DTPA-NLS-CSL360 radioimmunoconjugates (RIC) recognize the overexpression of the interleukin-3 receptor α-subchain (CD123) relative to the β-subchain (CD131) on leukemia stem cells (LSC). Our aim was to study Auger electron radioimmunotherapy (RIT) of acute myeloid leukemia (AML) with (111)In-DTPA-NLS-CSL360 in non-obese diabetic severe combined immunodeficiency (NOD/SCID) mice or NOD-Rag1(null)IL2rγ(null) (NRG) mice engrafted with CD123(+) human AML-5 cells. METHODS: The toxicity of three doses of (111)In-DTPA-NLS-CSL360 (3...
October 2016: Nuclear Medicine and Biology
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