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Nuclear Medicine and Biology

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https://www.readbyqxmd.com/read/28327434/-99m-tc-3prgd2-scintigraphy-to-stage-liver-fibrosis-and-evaluate-reversal-after-fibrotic-stimulus-withdrawn
#1
Xin Zhang, Qiyong Guo, Yu Shi, Weina Xu, Shupeng Yu, Zhiguang Yang, Li Cao, Changping Liu, Zhoushe Zhao, Jun Xin
OBJECTIVE: Scintigraphy using 99mTc-3PRGD2 targeting integrin αvβ3 could assess activation of hepatic stellate cells (HSCs). Liver fibrogenesis is intimately associated with activation of HSCs, and the fibrolytic process is accompanied by the reduction of the activated HSCs. In this study, we aimed to evaluate the feasibility of this method to assess the severity of liver fibrosis and the reversal after the fibrotic stimulus withdrawal. METHODS: Liver fibrosis of different stages was induced by thioacetamide (TAA) injection for 2, 4 and 6 weeks (n = 6 for each time point)...
March 7, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28292697/excitation-function-and-yield-for-the-103-rh-d-2n-103-pd-nuclear-reaction-optimization-of-the-production-of-palladium-103
#2
Simone Manenti, María Del Carmen Alí Santoro, Giulio Cotogno, Charlotte Duchemin, Ferid Haddad, Uwe Holzwarth, Flavia Groppi
Deuteron-induced nuclear reactions for the generation of (103)Pd were investigated using the stacked-foil activation technique on rhodium targets at deuteron energies up to Ed=33MeV. The excitation functions of the reactions (103)Rh(d,xn)(101,103)Pd, (103)Rh(d,x)(100g,cum,101m,g,102m,g)Rh and (103)Rh(d,2p)(103)Ru have been measured, and the Thick-Target Yield for (103)Pd has been calculated.
March 6, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28288384/bulk-production-and-evaluation-of-high-specific-activity-186g-re-for-cancer-therapy-using-enriched-186-wo3-targets-in-a-proton-beam
#3
Tara Mastren, Valery Radchenko, Hong T Bach, Ethan R Balkin, Eva R Birnbaum, Mark Brugh, Jonathan W Engle, Matthew D Gott, James Guthrie, Heather M Hennkens, Kevin D John, Alan R Ketring, Marina Kuchuk, Joel R Maassen, Cleo M Naranjo, F Meiring Nortier, Tim E Phelps, Silvia S Jurisson, D Scott Wilbur, Michael E Fassbender
INTRODUCTION: Rhenium-186g (t1/2 = 3.72 d) is a β(-) emitting isotope suitable for theranostic applications. Current production methods rely on reactor production by way of the reaction (185)Re(n,γ)(186g)Re, which results in low specific activities limiting its use for cancer therapy. Production via charged particle activation of enriched (186)W results in a (186g)Re product with a higher specific activity, allowing it to be used more broadly for targeted radiotherapy applications. This targets the unmet clinical need for more efficient radiotherapeutics...
March 3, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28301817/simple-and-rapid-radiosynthesis-of-n-18-f-labeled-glutamic-acid-as-a-hepatocellular-carcinoma-pet-tracer
#4
Aixia Sun, Shaoyu Liu, Xiaolan Tang, Dahong Nie, Ganghua Tang, Zhanwen Zhang, Fuhua Wen, Xiaoyan Wang
INTRODUCTION: We have reported that N-(2-(18)F-fluoropropionyl)-L-glutamate ((18)F-FPGLU) showed good tumor-to-background contrast and (18)F-FPGLU was prepared via complex multi-step reaction sequence; here, it is synthesized by a facile two-step reaction sequence. The objectives of this study are to synthesize (18)F-FPGLU via a two-step reaction sequence and to evaluate the value of (18)F-FPGLU in nude mice bearing human hepatocellular carcinoma SMCC-7721 (HCC SMCC-7721). METHODS: (18)F-FPGLU was synthetized from the precursor (2S)-dimethyl 2-(2-bromopropanamido)pentanedioate via the two-step on-column hydrolysis using a modified commercial FDG synthesizer...
March 2, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28288383/effect-of-methoxy-group-position-on-biological-properties-of-18-f-labeled-benzyl-triphenylphosphonium-cations
#5
Shuting Chen, Zuoquan Zhao, Ying Zhang, Wei Fang, Jie Lu, Xianzhong Zhang
INTRODUCTION: (18)F-labeled phosphonium cations targeting mitochondrial membrane potential would be promising for positron emission tomography (PET) myocardial perfusion imaging (MPI). The purpose of this study was to examine the influence of additional methoxy group and its different positions on myocardium uptake and pharmacokinetics properties of (18)F-labeled benzyl triphenylphosphonium cations. METHOD: In this study, three novel (18)F-labeled phosphonium cations, [(18)F]4-(fluoromethyl)benzyltris(4-methoxyphenyl) phosphonium cation (1b), [(18)F]4-(fluoromethyl)benzyltris(2-methoxyphenyl) phosphonium cation (2b) and [(18)F]4-(fluoromethyl)benzyltris(3-methoxyphenyl) phosphonium cation (3b), were efficiently prepared by a One-Pot method starting from the substitution of non-carried-added fluoride-18...
February 24, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28279906/preparation-and-evaluation-of-rhenium-188-pamidronate-as-a-palliative-treatment-in-bone-metastasis
#6
Mostafa Erfani, Nasim Rahmani, Alireza Doroudi, Mohammad Shafiei
OBJECTIVE: Rhenium-188-hydroxyethylidene diphosphonate ((188)Re-HEDP) as a first generation bisphosphonate has been widely used for bone seeking radiopharmaceutical in cases of metastatic bone disease. No study has been yet reported on preparing a complex of (188)Re with pamidronate (3-aminohydroxypropylidene-1,1-bisphosphonic acid) (PMA) as a second generation bisphosphonate. Based on this fact, it was hypothesized that a bone-seeking (188)Re-PMA radiopharmaceutical could be developed as an agent for palliative radiotherapy of bone pain due to skeletal metastases...
February 24, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28254656/gefitinib-enhances-radiotherapeutic-effects-of-131-i-hegf-targeted-to-egfr-by-increasing-tumor-uptake-of-hegf-in-tumor-xenografts
#7
Lu Xia, He Peng, Luo Zhiqiang, Zhang Xiaoli
Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor which has been proven effective for cancer treatment. In this study, we sought to determine whether gefitinib could increase the in vivo tumor uptake of human (131)I-EGF ((131)I-hEGF), thereby enhancing the potential of hEGF as a vehicle for EGFR-targeted radionuclide therapy. Western blot analysis was conducted to detect the effects of gefitinib on EGFR expression in human head and neck squamous carcinoma cell line UM-SCC-22B...
February 4, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28193503/clinical-translation-of-a-psma-inhibitor-for-99m-tc-based-spect
#8
Guillermina Ferro-Flores, Myrna Luna-Gutiérrez, Blanca Ocampo-García, Clara Santos-Cuevas, Erika Azorín-Vega, Nallely Jiménez-Mancilla, Emmanuel Orocio-Rodríguez, Jenny Davanzo, Francisco O García-Pérez
BACKGROUND: Prostate-specific membrane antigen (PSMA) is highly over-expressed in advanced prostate cancers. (68)Ga-labeled PSMA inhibitors (iPSMA) are currently used for prostate cancer detection by PET imaging. The availability of simple, efficient and reproducible radiolabeling procedures is essential for developing new SPECT radiopharmaceuticals for clinical translation. The aim of this research was to prepare (99m)Tc-EDDA/HYNIC-Lys(Nal)-Urea-Glu ((99m)Tc-EDDA/HYNIC-iPSMA) obtained from lyophilized kit formulations and evaluate the in vitro and in vivo radiopharmaceutical binding to prostate cancer cells over-expressing PSMA, as well as the (99m)Tc-EDDA/HYNIC-iPSMA normal biodistribution in humans and the preliminary uptake in patients with prostate cancer...
February 3, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28193502/development-of-a-preclinical-211-rn-211-at-generator-system-for-targeted-alpha-therapy-research-with-211-at
#9
Jason R Crawford, Hua Yang, Peter Kunz, D Scott Wilbur, Paul Schaffer, Thomas J Ruth
INTRODUCTION: The availability of (211)At for targeted alpha therapy research can be increased by the (211)Rn/(211)At generator system, whereby (211)At is produced by (211)Rn electron capture decay. This study demonstrated the feasibility of using generator-produced (211)At to label monoclonal antibody (BC8, anti-human CD45) for preclinical use, following isolation from the (207)Po contamination also produced by these generators (by (211)Rn α-decay). METHODS: (211)Rn was produced by (211)Fr electron capture decay following mass separated ion beam implantation and chemically isolated in liquid alkane hydrocarbon (dodecane)...
January 29, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28273495/-99m-tc-labeling-and-evaluation-of-a-hynic-modified-small-molecular-inhibitor-of-prostate-specific-membrane-antigen
#10
Xiaoping Xu, Jianping Zhang, Silong Hu, Simin He, Xiao Bao, Guang Ma, Jianmin Luo, Jingyi Cheng, Yingjian Zhang
INTRODUCTION: Prostate-specific membrane antigen (PSMA) is a well-established target in the development of radiopharmaceuticals for the diagnosis and therapy of prostate cancer (PCa). In this study, we evaluated a novel (99m)Tc-labeled small molecular inhibitor of PSMA. METHODS: This new small-molecular inhibitor of PSMA, 6-hydrazinonicotinate-Aminocaproic acid-Lysine-Urea-Glutamate (HYNIC-ALUG) was radiolabeled by (99m)Tc and was evaluated both in vitro and in vivo using PCa models (PC-3 and LNCaP)...
January 28, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28284101/relationship-between-14-c-meaib-uptake-and-amino-acid-transporter-family-gene-expression-levels-or-proliferative-activity-in-a-pilot-study-in-human-carcinoma-cells-comparison-with-3-h-methionine-uptake
#11
Shinya Kagawa, Ryuichi Nishii, Tatsuya Higashi, Hiroshi Yamauchi, Emi Ogawa, Hiroyuki Okudaira, Masato Kobayashi, Mitsuyoshi Yoshimoto, Naoto Shikano, Keiichi Kawai
INTRODUCTION: To clarify the difference between system A and L amino acid transport imaging in PET clinical imaging, we focused on the use of α-[N-methyl-(11)C]-methylaminoisobutyric acid ([(11)C]MeAIB), and compared it with [S-methyl-(11)C]-L-methionine ([(11)C]MET). The aim of this study was to assess the correlation of accumulation of these two radioactive amino acid analogs with expression of amino acid transporters and cell proliferative activity in carcinoma cells. METHODS: Amino acid uptake inhibitor studies were performed in four human carcinoma cells (epidermal carcinoma A431, colorectal carcinoma LS180, and lung carcinomas PC14/GL and H441/GL) using the radioisotope analogs [(3)H]MET and [(14)C]MeAIB...
January 26, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28208058/monitoring-of-macrophage-accumulation-in-statin-treated-atherosclerotic-mouse-model-using-sodium-iodide-symporter-imaging-system
#12
Ran Ji Yoo, Min Hwan Kim, Sang-Keun Woo, Kwang Il Kim, Tae Sup Lee, Yang-Kyu Choi, Joo Hyun Kang, Sang Moo Lim, Yong Jin Lee
INTRODUCTION: Macrophages play a key role in atherosclerotic plaque formation in atherosclerosis, but its detailed understanding has poorly investigated until now. Thus, we sought to demonstrate a noninvasive technique for macrophage tracking to atherosclerotic lesions in apolipoprotein E(-/-)(ApoE(-/-)) mice with an imaging system based on sodium iodide symporter (NIS) gene coupled with (99m)Tc-single-photon emission computed tomography (SPECT). METHODS AND RESULTS: Macrophage cells (RAW264...
January 25, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28157625/iminodiacetic-acid-as-bifunctional-linker-for-dimerization-of-cyclic-rgd-peptides
#13
Dong Xu, Zuo-Quan Zhao, Shu-Ting Chen, Yong Yang, Wei Fang, Shuang Liu
INTRODUCTION: In this study, I2P-RGD2 was used as the example to illustrate a novel approach for dimerization of cyclic RGD peptides. The main objective of this study was to explore the impact of bifunctional linkers (glutamic acid vs. iminodiacetic acid) on tumor-targeting capability and excretion kinetics of the (99m)Tc-labeled dimeric cyclic RGD peptides. METHODS: HYNIC-I2P-RGD2 was prepared by reacting I2P-RGD2 with HYNIC-OSu in the presence of diisopropylethylamine, and was evaluated for its αvβ3 binding affinity against (125)I-echistatin bound to U87MG glioma cells...
January 20, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28237630/-18-f-fluoro-2-deoxyglucose-pet-informs-neutrophil-accumulation-and-activation-in-lipopolysaccharide-induced-acute-lung-injury
#14
Rosana S Rodrigues, Fernando A Bozza, Christopher J Hanrahan, Li-Ming Wang, Qi Wu, John M Hoffman, Guy A Zimmerman, Kathryn A Morton
INTRODUCTION: Molecular imaging of the earliest events related to the development of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) could facilitate therapeutic development and patient management. We previously reported that (18)F-fluoro-2-deoxyglucose ((18)F-FDG) PET identifies ALI/ARDS prior to radiographic abnormalities. The purpose of this study was to establish the time courses of (18)F-FDG uptake, edema and neutrophil recruitment in an endotoxin-induced acute lung injury model and to examine molecular events required for (14)C-2DG uptake in activated neutrophils...
January 17, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28160666/redesign-of-negatively-charged-111-in-dtpa-octreotide-derivative-to-reduce-renal-radioactivity
#15
Nobuhiro Oshima, Hiromichi Akizawa, Hidekazu Kawashima, Songji Zhao, Yan Zhao, Ken-Ichi Nishijima, Yoji Kitamura, Yasushi Arano, Yuji Kuge, Kazue Ohkura
INTRODUCTION: Radiolabeled octreotide derivatives have been studied as diagnostic and therapeutic agents for somatostatin receptor-positive tumors. To prevent unnecessary radiation exposure during their clinical application, the present study aimed to develop radiolabeled peptides which could reduce radioactivity levels in the kidney at both early and late post-injection time points by introducing a negative charge with an acidic amino acid such as L-aspartic acid (Asp) at a suitable position in (111)In-DTPA-conjugated octreotide derivatives...
January 17, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28157626/evaluation-of-18-f-atri-as-pet-tracer-for-in-vivo-imaging-of-atr-in-mouse-models-of-brain-cancer
#16
Giuseppe Carlucci, Brandon Carney, Ahmad Sadique, Axel Vansteene, Jun Tang, Thomas Reiner
RATIONALE: Ataxia telangiectasia and Rad3-related (ATR) threonine serine kinase is one of the key elements in orchestrating the DNA damage response (DDR). As such, inhibition of ATR can amplify the effects of chemo- and radiation-therapy, and several ATR inhibitors (ATRi) have already undergone clinical testing in cancer. For more accurate patient selection, monitoring and staging, real-time in vivo imaging of ATR could be invaluable; the development of appropriate imaging agents has remained a major challenge...
January 16, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28126683/pet-imaging-of-64-cu-dota-scfv-anti-psma-lipid-nanoparticles-lnps-enhanced-tumor-targeting-over-anti-psma-scfv-or-untargeted-lnps
#17
Patty Wong, Lin Li, Junie Chea, Melissa K Delgado, Desiree Crow, Erasmus Poku, Barbara Szpikowska, Nicole Bowles, Divya Channappa, David Colcher, Jeffrey Y C Wong, John E Shively, Paul J Yazaki
INTRODUCTION: Single chain (scFv) antibodies are ideal targeting ligands due to their modular structure, high antigen specificity and affinity. These monovalent ligands display rapid tumor targeting but have limitations due to their fast urinary clearance. METHODS: An anti-prostate membrane antigen (PSMA) scFv with a site-specific cysteine was expressed and evaluated in a prostate cancer xenograft model by Cu-64 PET imaging. To enhance tumor accumulation, the scFv-cys was conjugated to the co-polymer DSPE-PEG-maleimide that spontaneously assembled into a homogeneous multivalent lipid nanoparticle (LNP)...
April 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28126682/a-multi-species-evaluation-of-the-radiation-dosimetry-of-11-c-erlotinib-the-radiolabeled-analog-of-a-clinically-utilized-tyrosine-kinase-inhibitor
#18
J Ryan Petrulli, Søren B Hansen, Galith Abourbeh, Maqsood Yaqub, Idris Bahce, Daniel Holden, Yiyun Huang, Nabeel B Nabulsi, Joseph N Contessa, Eyal Mishani, Adriaan A Lammertsma, Evan D Morris
INTRODUCTION: Erlotinib is a tyrosine kinase inhibitor prescribed for non-small cell lung cancer (NSCLC) patients bearing epidermal growth factor receptor mutations in the kinase domain. The objectives of this study were to (1) establish a human dosimetry profile of [(11)C]erlotinib and (2) assess the consistency of calculated equivalent dose across species using the same dosimetry model. METHODS: Subjects examined in this multi-species study included: a stage IIIa NSCLC patient, 3 rhesus macaque monkeys, a landrace pig, and 4 athymic nude-Fox1nu mice...
April 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28110124/monoanionic-99m-tc-tricarbonyl-aminopolycarboxylate-complexes-with-uncharged-pendant-groups-radiosynthesis-and-evaluation-as-potential-renal-tubular-tracers
#19
Malgorzata Lipowska, Jeffrey Klenc, Nashwa Jarkas, Luigi G Marzilli, Andrew T Taylor
INTRODUCTION: (99m)Tc(CO)3-nitrilotriacetic acid, (99m)Tc(CO)3(NTA), is a new renal tubular agent with pharmacokinetic properties comparable to those of (131)I-OIH but the clearance of (99m)Tc(CO)3(NTA) and (131)I-OIH is still less than the clearance of PAH, the gold standard for the measurement of effective renal plasma flow. At physiological pH, dianionic (99m)Tc(CO)3(NTA) has a mononegative inner metal-coordination sphere and a mononegative uncoordinated carboxyl group. To evaluate alternate synthetic approaches, we assessed the importance of an uncoordinated carboxyl group, long considered essential for tubular transport, by evaluating the pharmacokinetics of three analogs with the (99m)Tc(CO)3(NTA) metal-coordination sphere but with uncharged pendant groups...
April 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28110123/investigation-of-123-i-production-using-electron-accelerator
#20
Albert Avetisyan, Robert Avagyan, Ruben Dallakyan, Gohar Avdalyan, Nikolay Dobrovolsky, Vasak Gavalyan, Ivetta Kerobyan, Gevorg Harutyunyan
The possibility of (123)I isotope production with the help of the high-intensity bremsstrahlung photons produced by the electron beam of the LUE50 linear electron accelerator at the A.I. Alikhanyan National Science Laboratory (Yerevan Physics Institute [YerPhI]) is considered. The production method has been established and shown to be successful. The (124)Xe(γ,n)(123)Xe→(123)I nuclear reaction has been investigated and the cross-section was calculated by nuclear codes TALYS 1.6 and EMPIRE 3.2. The optimum parameter of the thickness of the target was determined by GEANT4 code...
April 2017: Nuclear Medicine and Biology
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